Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
25208097 183330 3 None -1 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 183330 3 None -1 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
3917 3855 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1631926 207065 0 None - 1 Mouse 10.4 pEC50 = 10.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631926 207065 0 None - 1 Mouse 10.4 pEC50 = 10.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL264846 208877 0 None 12 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388462 161292 0 None 6 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None 6 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16131448 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1681 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1688 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
44361543 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
56947112 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
CHEMBL396460 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
16131448 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44388461 159281 0 None 6 3 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None 6 3 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
24822630 97401 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL272215 97401 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL593215 97401 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
16131448 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL409204 210994 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL261997 208769 6 None - 1 Human 9.8 pEC50 = 9.8 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL2372052 208419 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
16131448 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1681 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1688 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
44361543 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
56947112 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL396460 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL265801 208908 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010221v
16131448 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1681 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1688 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44361543 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
56947112 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
CHEMBL396460 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44388466 96041 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 96041 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL412537 211245 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1cccc(F)c1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL405648 210815 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL1627325 207058 0 None -8 8 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
CHEMBL427791 211624 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44388467 168828 0 None 4 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 168828 0 None 4 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
1682 2799 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
6324645 2799 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 2799 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL1631909 207059 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631909 207059 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
16131448 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1681 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1688 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
44361543 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
56947112 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
CHEMBL396460 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
12419 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
16131448 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1681 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1688 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44361543 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
56947112 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL396460 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44388462 161292 0 None -6 3 Mouse 9.4 pEC50 = 9.4 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None -6 3 Mouse 9.4 pEC50 = 9.4 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL263588 208824 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25208097 183330 3 None -1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481366 183330 3 None -1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
1682 2799 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
6324645 2799 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL384755 2799 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
3917 3855 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL429363 211768 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL1631923 207063 0 None - 1 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm101139f
CHEMBL1631923 207063 0 None - 1 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm101139f
3917 3855 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1162359 206765 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44388461 159281 0 None -6 3 Mouse 9.1 pEC50 = 9.1 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None -6 3 Mouse 9.1 pEC50 = 9.1 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414767 211396 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
1682 2799 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
6324645 2799 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2799 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
16131448 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL507847 212775 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631926 207065 0 None - 1 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose in presence of compound 14 by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose in presence of compound 14 by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL428668 211707 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1F)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44388467 168828 0 None -4 2 Mouse 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 168828 0 None -4 2 Mouse 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
44388462 161292 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16143911 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL511107 213807 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
1689 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
16131448 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1682 2799 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
6324645 2799 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 2799 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
44388461 159281 0 None -9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None -9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16131448 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL506825 212432 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
25207950 183204 0 None 120 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480426 183204 0 None 120 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
11956520 120041 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326228 120041 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545629 120041 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL556388 213948 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
CHEMBL559130 213956 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
25208095 190605 0 None 47 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL518950 190605 0 None 47 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL406097 210838 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Br)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
16131448 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
16131448 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1681 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1688 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
44361543 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
56947112 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL1162358 206764 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
25208101 183331 0 None 181 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481367 183331 0 None 181 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
25208245 183352 0 None 478 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481547 183352 0 None 478 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
25208099 187776 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL501331 187776 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
11464846 77226 19 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 77226 19 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL5073561 212518 0 None 107 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL264846 208877 0 None -12 3 Guinea pig 8.7 pEC50 = 8.7 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
CHEMBL437915 211981 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm010092i
CHEMBL5070802 212463 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5080536 212909 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5093093 213621 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL504872 212404 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL262224 208779 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None Cc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
9927928 90024 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387199 90024 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL507653 212663 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44574791 177992 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467119 177992 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
71624265 90013 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387188 90013 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL442305 212152 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL504540 212399 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL526352 213896 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 2799 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 2799 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 2799 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
76324308 102829 0 None 48 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084526 102829 0 None 48 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
16131448 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 2799 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 2799 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 2799 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
10406239 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326224 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326226 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3545624 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
56658044 65360 0 None -20 4 Human 7.0 pEC50 = 7.0 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834413 65360 0 None -20 4 Human 7.0 pEC50 = 7.0 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL5079432 212835 0 None -38 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)c1ccccc1 10.1021/acs.jmedchem.0c02062
CHEMBL442305 212152 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
9820782 142709 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389665 142709 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
9848990 188566 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial 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 4 2 5 4.4 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 10.1021/jm2003238
CHEMBL2368861 188566 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial 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 4 2 5 4.4 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 10.1021/jm2003238
CHEMBL511142 188566 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial 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 4 2 5 4.4 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 10.1021/jm2003238
134563650 169267 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439997 169267 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44426843 85286 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228964 85286 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
11164004 108051 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL320182 108051 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
10042904 206654 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL99738 206654 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL5078005 212746 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL525604 213871 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
10385808 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
8868 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
49843555 56995 0 None 288 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650844 56995 0 None 288 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL438398 212012 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCC(CC)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL437192 211950 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCCC(CCC)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9842289 119964 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354291 119964 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL389521 210670 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
1679 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11956680 120034 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325961 120034 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3545622 120034 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
134563655 173636 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 173636 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
9803475 77227 22 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 77227 22 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL5087383 213307 0 None -7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
90655976 110507 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262549 110507 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
118718276 114802 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349260 114802 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
22562137 90023 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387198 90023 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
118718277 114803 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349261 114803 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
16131448 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL389521 210670 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
25208247 183353 0 None 676 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481548 183353 0 None 676 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
11848225 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist 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 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist 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 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist 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 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist 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 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist 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 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
16131448 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL5086442 213246 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)cc1 10.1021/acs.jmedchem.0c02062
44430604 168195 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL437382 168195 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
53322001 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL1631924 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL265392 208889 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
46227961 13990 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198015 13990 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL593214 13990 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
44574705 178200 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468952 178200 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
71624269 90017 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387192 90017 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
129188462 175822 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4465668 175822 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4596017 175822 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10385808 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
53322001 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL1631924 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
42629117 177964 0 None 67 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466921 177964 0 None 67 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
122179052 120868 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581741 120868 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
76331525 102859 0 None 109 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084558 102859 0 None 109 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44430602 143910 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL390658 143910 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL556556 143910 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372051 208418 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372364 208418 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
81689704 120872 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581750 120872 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
16131448 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
9848990 188566 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 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 10.1021/acs.jmedchem.5b00130
CHEMBL2368861 188566 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 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 10.1021/acs.jmedchem.5b00130
CHEMBL511142 188566 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 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 10.1021/acs.jmedchem.5b00130
CHEMBL524873 213840 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
46227966 14049 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198704 14049 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611932 14049 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL389521 210670 0 None -11 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9954388 99065 1 None -4 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assay
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283480 99065 1 None -4 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assay
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL5081409 212965 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563496 173971 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4556227 173971 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
118718266 114792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349250 114792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL435511 211909 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
18782396 121157 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585388 121157 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586752 121157 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
44394284 65841 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184381 65841 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
44574588 177851 0 None 44 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466067 177851 0 None 44 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574585 178042 0 None 56 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL467488 178042 0 None 56 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
11451023 106725 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL316699 106725 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL268394 208995 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL396972 210744 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44394324 65809 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184234 65809 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
129188443 168959 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 168959 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
122179061 120879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581757 120879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44394283 65817 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184260 65817 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10155966 188678 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL511920 188678 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
44394375 123154 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL362160 123154 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
10139672 125354 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL364844 125354 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
53325608 56998 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650847 56998 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
44456216 154849 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL403588 154849 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL398224 210762 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCC(CC)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5093399 213640 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
3655995 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL320874 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
3655995 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
CHEMBL320874 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
134563699 175492 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4591048 175492 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44456187 95184 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL257921 95184 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
76320665 102850 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084549 102850 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL5070616 212460 0 None 20 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44456141 94897 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL256687 94897 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44430602 143910 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL390658 143910 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL556556 143910 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5081993 212999 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
9905428 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL505824 212416 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL264846 208877 0 None -17 3 Mouse 8.6 pEC50 = 8.6 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25207948 183203 0 None 18 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480425 183203 0 None 18 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL5074745 212549 0 None 15 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02062
CHEMBL499157 212310 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL5081578 212972 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44248674 102912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084677 102912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45271534 193576 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551111 193576 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45268153 194450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL561115 194450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45269032 194500 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
CHEMBL561373 194500 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
44247589 102832 0 None 37 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084529 102832 0 None 37 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46227963 14046 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198701 14046 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611929 14046 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
9905428 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
9925137 120038 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326222 120038 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3545626 120038 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
44394419 65864 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184451 65864 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
101886205 121160 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585402 121160 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586792 121160 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
1684 3298 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 3298 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 3298 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
16131448 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
86279209 110502 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262544 110502 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL405645 210812 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
44394381 66631 0 None 25 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL186822 66631 0 None 25 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL507269 212505 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL384866 210582 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
9844540 85278 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228911 85278 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
10274330 66325 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL185415 66325 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
9863568 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
53316968 56992 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650841 56992 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
44456296 97258 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL271478 97258 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44456298 168227 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL437601 168227 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL2372051 208418 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372364 208418 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
122179060 120878 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581756 120878 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
122179064 120882 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581762 120882 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL405645 210812 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL427954 211638 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(N)=O 10.1016/j.bmcl.2006.04.086
54756990 65358 0 None -2754 3 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834411 65358 0 None -2754 3 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
16131448 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1681 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1688 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
44361543 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
56947112 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL5085090 213165 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563704 176050 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4451073 176050 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4597933 176050 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
16131448 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL424934 211569 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
CHEMBL415781 211442 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL262928 208798 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
10109899 85269 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228857 85269 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL5094655 213719 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
9803475 77227 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
CHEMBL2088036 77227 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
10042904 162759 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL418980 162759 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL266667 208938 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
10042904 90012 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387187 90012 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL5094439 213709 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
25235412 102830 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084527 102830 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
25235412 114818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349276 114818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44430588 86391 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL232245 86391 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL541911 86391 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44456220 154888 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL403807 154888 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
22558157 110505 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262547 110505 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
16665918 79324 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211722 79324 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
134578342 172482 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
CHEMBL4519453 172482 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
44181744 102885 8 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 102885 8 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
11461888 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
11461888 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL405948 210830 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
9863568 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL3809510 210518 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL394588 210720 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCCC(CCC)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL442113 212149 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL1631922 207062 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC1=O 10.1021/jm101139f
CHEMBL1631922 207062 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC1=O 10.1021/jm101139f
25208249 183373 0 None 1202 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481707 183373 0 None 1202 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL555757 213945 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 213894 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL558807 213955 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
16131448 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44551464 14048 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198703 14048 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611931 14048 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL5079758 212856 0 None 151 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL1631921 207061 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm101139f
1641 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
3829 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
5497186 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL567175 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL406718 210860 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
16131448 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL455289 212239 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631925 207064 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631925 207064 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL5081139 212944 0 None 12 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
71624387 90020 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387195 90020 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
10134217 65929 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184698 65929 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL269029 209020 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL269029 209020 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL265544 208898 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44456185 166057 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL428076 166057 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
5268 3586 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
53 3586 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL300555 3586 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL505873 212418 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
10137876 124516 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364398 124516 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
9863568 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
122179056 120874 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581752 120874 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
10110916 65915 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184646 65915 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44394487 65100 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182967 65100 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
134563466 170716 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4460695 170716 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574789 177963 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
CHEMBL466919 177963 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
16131448 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1631920 207060 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631920 207060 0 None - 1 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm101139f
53316969 57001 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650851 57001 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL5091985 213555 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
10385808 65796 0 None 38 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 38 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
53322245 56999 0 None 9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650848 56999 0 None 9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
9885005 57228 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL166387 57228 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
15512229 3321 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptorTested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
8864 3321 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptorTested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
CHEMBL355202 3321 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptorTested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
1682 2799 15 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
6324645 2799 15 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL384755 2799 15 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL500773 212346 0 None - 1 Rat 8.4 pEC50 = 8.4 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631921 207061 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm101139f
CHEMBL5081993 212999 0 None -2 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL505632 212414 0 None - 1 Rat 8.4 pEC50 = 8.4 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1162357 206763 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL443591 212168 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm010092i
CHEMBL394774 210722 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
3917 3855 0 None -28 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None -28 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None -28 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44388474 160483 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL411649 160483 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
10022859 98700 1 None 63 2 Human 7.4 pEC50 = 7.4 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
CHEMBL281274 98700 1 None 63 2 Human 7.4 pEC50 = 7.4 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
CHEMBL5070145 212446 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
90655973 110503 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262545 110503 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL219144 207653 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
122179050 120867 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581740 120867 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
16007142 138810 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
CHEMBL379297 138810 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
122179585 121159 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 381 2 1 4 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3cccc(F)c31)CC2 10.1039/C4MD00082J
CHEMBL3585401 121159 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 381 2 1 4 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3cccc(F)c31)CC2 10.1039/C4MD00082J
CHEMBL3586789 121159 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 381 2 1 4 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3cccc(F)c31)CC2 10.1039/C4MD00082J
12986253 120028 0 None -3 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325881 120028 0 None -3 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545610 120028 0 None -3 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL406010 210834 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)CNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
76316935 102833 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084530 102833 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44456140 168138 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL436852 168138 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
134578506 173718 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4550088 173718 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
101886199 121158 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585403 121158 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586777 121158 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
73350483 90018 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387193 90018 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
44456299 97017 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270216 97017 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44430590 160765 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL412461 160765 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL557791 160765 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
155542684 172568 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4521436 172568 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574629 188243 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL506634 188243 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL5072525 212501 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5090780 213496 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
118718291 114817 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349275 114817 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44394405 64221 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL181545 64221 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44394344 65833 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184328 65833 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
16131448 2796 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
1681 2796 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
1688 2796 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
44361543 2796 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
56947112 2796 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2796 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
16131448 2796 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
1681 2796 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
1688 2796 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
44361543 2796 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
56947112 2796 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2796 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
16131448 2796 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
25207946 190694 0 None 275 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL519100 190694 0 None 275 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL503512 212388 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 212400 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 212400 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
CHEMBL510117 213795 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44574586 188724 0 None 33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL512411 188724 0 None 33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574672 188785 0 None 10 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512950 188785 0 None 10 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL510117 213795 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist 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 None None None None 10.1016/j.bmc.2009.06.015
90655974 110504 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262546 110504 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
10714523 98637 1 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
CHEMBL280827 98637 1 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
44455999 97049 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL270394 97049 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
90655972 110501 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262543 110501 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
53319617 57000 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650849 57000 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL5073730 212521 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563691 170485 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4457077 170485 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574743 178016 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467313 178016 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
129188459 174586 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4570328 174586 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
71624270 90019 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387194 90019 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
44430588 86391 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL232245 86391 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL541911 86391 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5086409 213245 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL413944 211345 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44413442 79518 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
CHEMBL212575 79518 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
44394559 65961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184865 65961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL5092388 213581 0 None -8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134578456 171561 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4473045 171561 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
1682 2799 15 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
6324645 2799 15 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL384755 2799 15 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
11848793 188725 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512414 188725 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
24800107 191255 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
CHEMBL519925 191255 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
71624388 90022 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387197 90022 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
24798598 112078 7 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3301613 112078 7 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325959 112078 7 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL5072270 212496 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL442305 212152 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL427954 211638 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(N)=O 10.1016/j.bmcl.2006.04.086
44574631 177924 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466679 177924 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
76324309 102834 0 None 6 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084531 102834 0 None 6 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL234724 207783 0 None - 1 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5075880 212621 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL415583 211433 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None COc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
16131448 2796 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1681 2796 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1688 2796 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
44361543 2796 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
56947112 2796 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
CHEMBL396460 2796 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
129188454 169255 0 None 46 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439811 169255 0 None 46 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL5081432 212966 0 None 12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5092204 213568 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
146034955 174056 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 399 5 1 5 3.9 CCn1c(=O)n([C@@H]2CCN(C3CCC(C(C)C)CC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4558048 174056 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 399 5 1 5 3.9 CCn1c(=O)n([C@@H]2CCN(C3CCC(C(C)C)CC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
CHEMBL410167 211046 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(I)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
122179053 120870 0 None -33 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581743 120870 0 None -33 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44430605 165840 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1835 63 30 26 -10.9 CCC(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL427699 165840 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1835 63 30 26 -10.9 CCC(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
1682 2799 15 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
6324645 2799 15 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2799 15 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
90655978 110509 0 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262551 110509 0 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
146034954 170432 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 425 5 1 5 4.3 CCn1c(=O)n([C@@H]2CCN(CC3CCCC4CCCCC43)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4456531 170432 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 425 5 1 5 4.3 CCn1c(=O)n([C@@H]2CCN(CC3CCCC4CCCCC43)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
44332117 107402 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
CHEMBL319307 107402 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
44430590 160765 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL412461 160765 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL557791 160765 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44574744 188708 0 None 60 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512258 188708 0 None 60 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
10160920 66624 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL186773 66624 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
56664973 65355 0 None -12 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
CHEMBL1834409 65355 0 None -12 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
9997843 99191 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL284414 99191 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
16131448 2796 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1681 2796 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1688 2796 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
44361543 2796 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
56947112 2796 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL396460 2796 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL436819 211930 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9799433 90021 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387196 90021 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
53324890 56993 0 None 138 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650842 56993 0 None 138 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
16131448 2796 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL233069 207775 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
90655975 110506 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262548 110506 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
71624268 90016 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387191 90016 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
71624266 90014 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387189 90014 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL394775 210723 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
90655971 110500 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262542 110500 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL5081900 212992 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL504461 212397 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
76335144 102852 0 None 43 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084551 102852 0 None 43 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
9947044 97806 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL27460 97806 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL526142 213887 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
24824635 158265 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL409458 158265 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611933 158265 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL524339 213818 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
53319615 56994 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650843 56994 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL5085161 213169 0 None 89 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44574587 177850 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
CHEMBL466066 177850 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
11393860 4369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
CHEMBL101676 4369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
CHEMBL442305 212152 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
44596170 14047 0 None -933 4 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198702 14047 0 None -933 4 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611930 14047 0 None -933 4 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
71624389 90025 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387200 90025 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
134578457 173373 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4541337 173373 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44456412 97022 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270231 97022 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL219144 207653 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
16131448 2796 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2796 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2796 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2796 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2796 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2796 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11511090 73690 0 None 5888 3 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL202225 73690 0 None 5888 3 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
10296561 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
7361 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL201945 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
44143431 177921 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL466648 177921 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
44143431 177921 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL466648 177921 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
44143450 188220 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL506207 188220 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143456 178010 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467279 178010 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45273531 193242 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL541511 193242 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
45270907 194076 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557623 194076 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
24857819 186924 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL494350 186924 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
24857819 186924 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL494350 186924 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
24857820 96224 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL263918 96224 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
24857820 96224 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263918 96224 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143432 178123 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL468302 178123 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143432 178123 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468302 178123 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143453 177896 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466448 177896 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143455 177875 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466252 177875 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45273546 194092 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557721 194092 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143428 178126 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468308 178126 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44143446 177871 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466222 177871 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
44143448 178071 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467677 178071 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143451 178128 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468315 178128 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143430 188788 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL512975 188788 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
9823363 177882 0 None 1047 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466308 177882 0 None 1047 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143433 177981 0 None 154 3 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467057 177981 0 None 154 3 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
1691 2067 14 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
5311194 2067 14 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
CHEMBL357076 2067 14 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
24894426 185175 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL486644 185175 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
44143449 178006 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467266 178006 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44450085 96223 0 None 47 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263917 96223 0 None 47 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
44437610 144974 0 None - 1 Human 8.0 pIC50 = 8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 144974 0 None - 1 Human 8.0 pIC50 = 8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44561518 188854 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL513585 188854 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
44437642 91307 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240941 91307 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
46879578 5945 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080463 5945 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44437644 91351 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241155 91351 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437617 154427 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL401248 154427 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44391133 64779 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL182410 64779 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
70682351 76295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064158 76295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
44391081 62262 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL178318 62262 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44143427 188886 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL513855 188886 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
11597677 73299 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
CHEMBL201805 73299 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
70690755 76283 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064130 76283 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
46879716 5949 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080483 5949 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
53318067 56123 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933707 56123 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631930 56123 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
44143418 186646 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL492585 186646 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
11326750 185717 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
CHEMBL487458 185717 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
70690760 76297 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064160 76297 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
53318067 56123 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933707 56123 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631930 56123 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
44437640 90787 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240086 90787 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
127034022 138461 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
CHEMBL3785605 138461 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
44437615 89932 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238637 89932 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437623 144635 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391234 144635 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44391094 64129 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181389 64129 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44437637 91451 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241357 91451 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
45270917 193363 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL549439 193363 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
10159203 65264 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183355 65264 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
70684436 76294 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064157 76294 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
44450208 95756 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260820 95756 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44391062 122096 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 122096 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44391062 122096 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 122096 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44189834 13893 0 None 1047 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197240 13893 0 None 1047 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563657 13893 0 None 1047 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44391067 63114 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
CHEMBL179797 63114 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
44437628 170088 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL445154 170088 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
46879538 6093 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081192 6093 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44189733 13901 3 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197275 13901 3 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL564840 13901 3 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44391157 64540 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182202 64540 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44437646 89899 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238602 89899 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437656 145170 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
CHEMBL391631 145170 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
44449766 155143 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL405078 155143 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44391103 65225 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
CHEMBL183135 65225 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
46879669 5877 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079942 5877 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
11462727 188781 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL512896 188781 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
135458466 79097 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL211390 79097 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
44143432 178122 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468301 178122 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45268355 194556 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL561732 194556 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
44576628 187134 0 None 6 4 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL495402 187134 0 None 6 4 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
45269358 194507 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561397 194507 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
45268498 195016 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
CHEMBL564812 195016 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
44143437 178049 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL467533 178049 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
45267505 194377 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560468 194377 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
45273537 194744 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL562932 194744 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
10199945 96225 0 None 42 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263919 96225 0 None 42 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45102745 5951 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080485 5951 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44143438 178146 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL468504 178146 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
44450086 157738 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
CHEMBL408901 157738 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
10451761 37753 0 None 38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
CHEMBL146013 37753 0 None 38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
10783436 37952 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
CHEMBL146191 37952 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
44437648 147088 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393138 147088 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
46879539 5405 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1076242 5405 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
22272877 95439 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL259185 95439 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
22272877 95439 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259185 95439 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
11516508 138457 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785560 138457 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44576625 186905 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL494219 186905 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
136043779 77744 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210292 77744 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11552010 138475 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
CHEMBL3785728 138475 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
70690757 76288 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064139 76288 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
136043782 138122 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL377736 138122 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
44437602 90209 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 90209 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44391155 64922 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182819 64922 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
44391134 122784 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL361576 122784 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
11602409 138582 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3786899 138582 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44437601 90183 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 90183 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
24894428 185735 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL487485 185735 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
44576627 192629 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL523724 192629 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44450210 95758 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260822 95758 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
46879670 5878 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079943 5878 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
127033703 138492 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3785952 138492 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
44189735 13894 0 None 363 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197249 13894 0 None 363 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563980 13894 0 None 363 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
136043759 78284 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211254 78284 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
10221539 156444 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL407325 156444 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
10221539 156444 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407325 156444 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143454 188576 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL511205 188576 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45270184 193590 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL551208 193590 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
22272974 96217 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263903 96217 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44437606 144973 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391486 144973 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
53316771 56121 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933706 56121 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631928 56121 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
53316771 56121 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933706 56121 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631928 56121 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
44437652 90182 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238819 90182 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437619 90783 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240074 90783 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
46879629 5781 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079417 5781 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
11626062 138407 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785095 138407 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44437613 146346 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL392548 146346 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10225083 165832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 165832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44143436 177881 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466307 177881 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
10225083 165832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL427683 165832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44450209 95757 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260821 95757 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
53319408 56120 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933705 56120 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631927 56120 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
53319408 56120 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933705 56120 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631927 56120 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
44437610 144974 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 144974 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44143452 178150 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468524 178150 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
11583016 73989 0 None 1698 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
CHEMBL202443 73989 0 None 1698 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
44143429 178149 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468518 178149 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44561020 178596 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL472304 178596 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
45273679 193952 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
CHEMBL556300 193952 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
44178080 194396 1 None 1584 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560667 194396 1 None 1584 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143419 187012 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494767 187012 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44437649 90181 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238818 90181 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44574003 177918 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL466631 177918 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
10301207 148111 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393960 148111 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
70688697 76296 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064159 76296 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
11525624 133003 0 None 181 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL370870 133003 0 None 181 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
136043800 77422 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209213 77422 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
10225083 165832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 165832 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437645 91352 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL241157 91352 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437605 90443 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239260 90443 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
70696991 76293 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064156 76293 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
46879478 5398 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076208 5398 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
136043780 138725 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL379048 138725 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
44574053 178036 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467473 178036 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143406 186906 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL494230 186906 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
70686573 76285 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 406 5 0 4 2.2 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064133 76285 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 406 5 0 4 2.2 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
11188910 188843 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
CHEMBL513423 188843 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
46879580 5776 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079400 5776 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44143435 177857 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466112 177857 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
44517710 194838 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL563593 194838 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
1691 2067 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
5311194 2067 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
CHEMBL357076 2067 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
11152739 188646 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
CHEMBL511658 188646 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
44391138 65117 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
CHEMBL182995 65117 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
46879537 6092 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081191 6092 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
11544795 138474 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785718 138474 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44437654 145190 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391650 145190 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437647 89898 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238600 89898 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
127034292 138536 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3786469 138536 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
45102745 5950 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080484 5950 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44576626 192753 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL525054 192753 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44143442 177917 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL466630 177917 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
45270082 193565 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL551002 193565 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
44437602 90209 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 90209 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
53323365 56122 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
CHEMBL1631929 56122 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
136043819 77568 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209537 77568 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
10225083 165832 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 165832 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
127034023 138611 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3787174 138611 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
46879667 5875 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079940 5875 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
17858448 95499 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259452 95499 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143457 178011 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467280 178011 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
11372427 178566 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
CHEMBL472125 178566 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
46879581 5808 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079571 5808 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44143434 177931 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466702 177931 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
53320710 56124 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933708 56124 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631931 56124 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
11633324 72318 0 None 724 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
CHEMBL199639 72318 0 None 724 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
53320710 56124 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933708 56124 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631931 56124 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
45272626 194081 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL557653 194081 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
44437610 144974 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 144974 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
53323365 56122 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
CHEMBL1631929 56122 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
44437630 145017 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391518 145017 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437602 90209 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 90209 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44450151 95335 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258711 95335 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44391104 64668 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182328 64668 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44437636 144894 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391422 144894 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
11619553 161159 0 None 407 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
CHEMBL413571 161159 0 None 407 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
44143445 177870 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466221 177870 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44391124 95978 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL262104 95978 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44437601 90183 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 90183 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437626 90178 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238795 90178 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
136043788 138800 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL379284 138800 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
11187225 178576 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL472168 178576 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
22273044 95334 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258710 95334 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
46879579 5946 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080464 5946 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
45269357 194506 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561396 194506 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
44437639 90786 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240085 90786 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437604 90210 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239045 90210 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
22272900 96213 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263889 96213 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44390989 165327 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL424971 165327 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
44391052 129134 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL367367 129134 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44437638 90785 0 None - 1 Human 7.0 pIC50 = 7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240084 90785 0 None - 1 Human 7.0 pIC50 = 7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
25001412 62307 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783826 62307 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL2372052 208419 0 None - 1 Guinea pig 9.5 pKd = 9.5 Functional
Antagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372052 208419 0 None - 1 Rat 9.2 pKd = 9.2 Functional
Antagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372052 208419 0 None - 1 Mouse 9.1 pKd = 9.1 Functional
Antagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAntagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
53320710 56124 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933708 56124 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631931 56124 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
25001412 62307 0 None - 0 Mouse 8.0 pKd = 8 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783826 62307 0 None - 0 Mouse 8.0 pKd = 8 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
127043001 139823 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808398 139823 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL269068 209022 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human NOP receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAntagonist activity at human NOP receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL269068 209022 0 None - 0 Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAntagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
127044528 139825 0 None - 1 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808415 139825 0 None - 1 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL269068 209022 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
10296561 1024 20 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
7361 1024 20 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL201945 1024 20 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
127043559 139967 0 None - 1 Human 6.3 pKd = 6.3 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3810104 139967 0 None - 1 Human 6.3 pKd = 6.3 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL269068 209022 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
127043364 139835 0 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808523 139835 0 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
44339596 9688 2 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL113684 9688 2 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
11743914 109164 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL322515 109164 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
44339424 9233 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.2 CC(C)C1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111192 9233 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.2 CC(C)C1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
44339695 9261 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 381 2 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(C2CCC3CCCCC3C2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111347 9261 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 381 2 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(C2CCC3CCCCC3C2)CC1 10.1016/s0960-894x(03)00665-6
44339425 8580 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 4 1 2 5.3 CCCC1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109563 8580 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 4 1 2 5.3 CCCC1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
44339374 110095 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL325536 110095 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
44339423 9239 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 5.9 CC(C)C1CCC(N2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111230 9239 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 5.9 CC(C)C1CCC(N2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
46227963 14046 0 None -3 4 Human 8.4 pKi = 8.4 Functional
Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS bindingAntagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198701 14046 0 None -3 4 Human 8.4 pKi = 8.4 Functional
Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS bindingAntagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611929 14046 0 None -3 4 Human 8.4 pKi = 8.4 Functional
Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS bindingAntagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
44339576 8625 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109598 8625 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
44339504 108344 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 335 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL320991 108344 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 335 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
44339684 9572 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 395 2 1 2 4.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(C2Cc3ccccc3C2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL112974 9572 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 395 2 1 2 4.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(C2Cc3ccccc3C2)CC1 10.1016/s0960-894x(03)00665-6
10499 3779 0 None - 1 Mouse 7.8 pA2 = 7.8 Functional
Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.
Guide to Pharmacology 397 5 1 5 4.1 OCC1=C(CCN(C1)CC1CCCCCCC1)n1c(=O)n(c2c1cccc2)CC 16202610
11494970 3779 0 None - 1 Mouse 7.8 pA2 = 7.8 Functional
Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.
Guide to Pharmacology 397 5 1 5 4.1 OCC1=C(CCN(C1)CC1CCCCCCC1)n1c(=O)n(c2c1cccc2)CC 16202610
CHEMBL3182208 3779 0 None - 1 Mouse 7.8 pA2 = 7.8 Functional
Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.
Guide to Pharmacology 397 5 1 5 4.1 OCC1=C(CCN(C1)CC1CCCCCCC1)n1c(=O)n(c2c1cccc2)CC 16202610
66553195 92699 29 None 1 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 None
CHEMBL2443262 92699 29 None 1 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 None
12419 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
24800108 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
CHEMBL481512 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
1684 3298 17 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
9844019 3298 17 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
CHEMBL2088034 3298 17 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
1686 3012 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 15743186
1679 266 21 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
9963005 266 21 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
CHEMBL437723 266 21 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
11597355 3485 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8869 3485 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
49843739 3598 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
8867 3598 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
CHEMBL3262554 3598 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
15512229 3321 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
8864 3321 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
CHEMBL355202 3321 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
11848225 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8868 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
8865 3175 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 24903280
1680 267 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
3917 3855 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
3917 3855 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
44430609 3855 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
44430609 3855 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
CHEMBL409969 3855 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
CHEMBL409969 3855 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
16131448 2796 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2796 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2796 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2796 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2796 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2796 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1691 2067 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
5311194 2067 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
CHEMBL357076 2067 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
10047612 3460 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
10047612 3460 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1693 3460 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
1693 3460 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
CHEMBL559569 3460 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
CHEMBL559569 3460 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
10296561 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
10296561 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
7361 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
7361 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
CHEMBL201945 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
CHEMBL201945 1024 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
10500 2773 0 None - 1 Human 7.4 pKB = 7.4 Functional
Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.
Guide to Pharmacology 512 6 1 5 3.8 NC(=O)Cn1c(C(=O)N2CCOCC2)c(c2c1cccc2)CN1CCC(CC1)c1c(F)cccc1Cl 22994368
24889797 2773 0 None - 1 Human 7.4 pKB = 7.4 Functional
Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.
Guide to Pharmacology 512 6 1 5 3.8 NC(=O)Cn1c(C(=O)N2CCOCC2)c(c2c1cccc2)CN1CCC(CC1)c1c(F)cccc1Cl 22994368


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
CHEMBL414542 211380 0 None - 1 Human 10.2 pEC50 = 10.2 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
44388462 161292 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL266191 208924 0 None - 1 Human 10.1 pEC50 = 10.1 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
162662480 181463 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4781235 181463 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL408356 210951 0 None - 1 Human 9.9 pEC50 = 9.9 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
44388461 159281 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL415845 211446 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
44388467 168828 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 168828 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL264084 208850 0 None - 1 Human 9.6 pEC50 = 9.6 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162662934 181435 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4780822 181435 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162676761 182924 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4799815 182924 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
124565311 173488 0 None 165 2 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4544227 173488 0 None 165 2 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL264846 208877 0 None - 1 Human 9.5 pEC50 = 9.5 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388474 160483 0 None - 1 Human 9.4 pEC50 = 9.4 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP) Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL411649 160483 0 None - 1 Human 9.4 pEC50 = 9.4 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP) Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
162676231 182734 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4797388 182734 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
16131448 2796 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1681 2796 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1688 2796 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
44361543 2796 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
56947112 2796 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
CHEMBL396460 2796 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
162656512 180315 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4757730 180315 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410979 211098 0 None - 1 Human 9.3 pEC50 = 9.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162651080 179630 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749802 179630 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162650489 179444 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747497 179444 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162669053 182135 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4789749 182135 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL438537 212016 0 None - 1 Human 9.1 pEC50 = 9.1 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
162676138 182806 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4798159 182806 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL263588 208824 0 None - 1 Human 9.1 pEC50 = 9.1 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388466 96041 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 96041 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL415584 211434 0 None - 1 Human 9.0 pEC50 = 9 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
16131448 2796 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 2796 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 2796 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 2796 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 2796 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2796 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
162661740 181252 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778484 181252 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406905 210872 0 None - 1 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162670125 182007 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4788218 182007 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162670701 182292 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792010 182292 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
10276738 171685 0 None 54 2 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assay
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4474536 171685 0 None 54 2 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assay
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
162645148 178827 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4740203 178827 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL265801 208908 0 None - 1 Human 8.7 pEC50 = 8.7 Binding
Binding of compound to cell membranes expressing human ORL1 receptor in HEk-293 cells using [32S]GTP-gamma-SBinding of compound to cell membranes expressing human ORL1 receptor in HEk-293 cells using [32S]GTP-gamma-S
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010092i
1682 2799 15 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
6324645 2799 15 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL384755 2799 15 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL405212 210793 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL439528 212086 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162653778 179889 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4753041 179889 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162652312 179730 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4751132 179730 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
162649797 179441 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747450 179441 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162650108 179551 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748849 179551 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
11848225 862 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 862 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 862 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3545616 862 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 862 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
162659015 180798 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4763461 180798 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162652312 179730 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4751132 179730 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL412479 211238 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None CC(C)C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.9b02057
162661740 181252 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778484 181252 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
11804490 181223 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778171 181223 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL2403216 208662 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None COc1ccc2[nH]cc([C@H](CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O)c2c1 10.1016/j.bmcl.2013.05.064
162650108 179551 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748849 179551 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL2403218 208664 16 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2013.05.064
11137032 180846 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4764102 180846 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
25208097 183330 3 None 5 4 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 183330 3 None 5 4 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
162661631 181286 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778926 181286 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL2403216 208662 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxoneActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxone
ChEMBL None None None COc1ccc2[nH]cc([C@H](CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O)c2c1 10.1016/j.bmcl.2013.05.064
162676138 182806 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4798159 182806 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650867 179613 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749620 179613 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
5311327 179846 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4752457 179846 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162662934 181435 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4780822 181435 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162665903 181737 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
CHEMBL4784371 181737 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
9905428 4328 12 None 21 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL101454 4328 12 None 21 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
162659601 180607 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4761103 180607 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162646448 179109 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743726 179109 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162651080 179630 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749802 179630 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
11137032 180846 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4764102 180846 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162655432 180089 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755353 180089 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162655941 180150 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755981 180150 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162648427 179371 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4746696 179371 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
162676761 182924 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4799815 182924 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
25208097 183330 3 None 5 4 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 183330 3 None 5 4 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
10832076 37803 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
CHEMBL146054 37803 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
10534521 182459 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4794113 182459 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650635 179506 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748275 179506 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162659601 180607 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4761103 180607 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671943 182342 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792616 182342 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162659015 180798 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4763461 180798 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162673971 182558 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795259 182558 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162669053 182135 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4789749 182135 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671943 182342 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792616 182342 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162656512 180315 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4757730 180315 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162670125 182007 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4788218 182007 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162676231 182734 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4797388 182734 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
10763594 160718 1 None 120 4 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL412098 160718 1 None 120 4 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
15512228 67399 0 None 8 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL1907858 67399 0 None 8 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
162661152 180933 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4765138 180933 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162649797 179441 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747450 179441 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162648962 179200 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4744757 179200 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657281 180382 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4758592 180382 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162655941 180150 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755981 180150 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL414541 211379 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162653778 179889 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4753041 179889 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL413429 211309 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
155544763 172774 0 None 7 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL4527189 172774 0 None 7 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
162645845 179085 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743479 179085 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
11804490 181223 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778171 181223 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650867 179613 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749620 179613 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162658205 180537 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760586 180537 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162645845 179085 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743479 179085 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406905 210872 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL414767 211396 0 None 154 2 Human 8.3 pEC50 = 8.3 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
CHEMBL436732 211929 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162657281 180382 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4758592 180382 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL413944 211345 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP) at 1 uMAgonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP) at 1 uM
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
10593778 98772 0 None 10 4 Human 6.3 pEC50 = 6.3 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
CHEMBL28172 98772 0 None 10 4 Human 6.3 pEC50 = 6.3 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
1682 2799 15 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
6324645 2799 15 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
CHEMBL384755 2799 15 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
CHEMBL414543 211381 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
5311327 179846 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4752457 179846 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650489 179444 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747497 179444 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162670701 182292 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792010 182292 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162672438 182635 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4796153 182635 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162662480 181463 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4781235 181463 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162665903 181737 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
CHEMBL4784371 181737 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
CHEMBL2403218 208664 16 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxoneActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxone
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2013.05.064
162648962 179200 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4744757 179200 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162672438 182635 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4796153 182635 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL412479 211238 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None CC(C)C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.9b02057
162645148 178827 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4740203 178827 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
16131448 2796 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
1681 2796 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
1688 2796 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
44361543 2796 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
56947112 2796 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
CHEMBL396460 2796 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
162655432 180089 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755353 180089 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10534521 182459 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4794113 182459 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
416359 101377 16 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
CHEMBL300616 101377 16 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
162661631 181286 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778926 181286 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671290 182236 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4791156 182236 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
162673058 182534 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795008 182534 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162673058 182534 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795008 182534 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162661152 180933 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4765138 180933 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162645528 179044 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4742892 179044 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162645528 179044 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4742892 179044 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
11583008 175280 4 None 213 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assay
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4585935 175280 4 None 213 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assay
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
162646448 179109 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743726 179109 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
1682 2799 15 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
6324645 2799 15 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL384755 2799 15 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL410396 211061 16 None 1 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650635 179506 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748275 179506 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671290 182236 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4791156 182236 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
162673971 182558 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795259 182558 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162648427 179371 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4746696 179371 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL429239 211760 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL427617 211598 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162658205 180537 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760586 180537 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
24882570 114620 0 None - 1 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 114620 0 None - 1 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 114620 0 None - 1 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL414736 211394 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
101354795 114622 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343949 114622 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
44416445 168775 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1847 62 28 25 -8.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCCNC(=O)CNC(=O)CNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
CHEMBL441930 168775 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1847 62 28 25 -8.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCCNC(=O)CNC(=O)CNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
16131448 2796 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2796 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2796 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2796 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2796 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2796 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL443591 212168 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm010092i
CHEMBL511107 213807 0 None - 0 Rat 9.8 pIC50 = 9.8 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL506825 212432 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
1689 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 2796 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
11511090 73690 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL202225 73690 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
16131448 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL556388 213948 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL559130 213956 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
10296561 1024 20 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
7361 1024 20 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL201945 1024 20 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL507847 212775 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL265801 208908 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010092i
16131448 2796 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
1681 2796 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
1688 2796 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
44361543 2796 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
56947112 2796 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
CHEMBL396460 2796 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
CHEMBL555757 213945 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 213894 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL558807 213955 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL500773 212346 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1682 2799 15 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
6324645 2799 15 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 2799 15 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
CHEMBL503512 212388 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 212400 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505632 212414 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 212400 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505824 212416 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL406718 210860 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
CHEMBL504872 212404 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44143431 177921 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL466648 177921 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
44143431 177921 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL466648 177921 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL437915 211981 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm010092i
CHEMBL499157 212310 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
155569742 176068 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 415 6 1 5 3.6 O=c1n(CCF)c2ccccc2n1[C@H]1CCN(C[C@H]2CCCCC23CC3)C[C@@H]1CO 10.1021/acs.jmedchem.5b01499
CHEMBL4454908 176068 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 415 6 1 5 3.6 O=c1n(CCF)c2ccccc2n1[C@H]1CCN(C[C@H]2CCCCC23CC3)C[C@@H]1CO 10.1021/acs.jmedchem.5b01499
CHEMBL4598052 176068 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 415 6 1 5 3.6 O=c1n(CCF)c2ccccc2n1[C@H]1CCN(C[C@H]2CCCCC23CC3)C[C@@H]1CO 10.1021/acs.jmedchem.5b01499
16131448 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2796 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
16131448 2796 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44456296 97258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL271478 97258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
16131448 2796 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1679 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
9963005 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
CHEMBL437723 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
44416444 161032 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1604 53 23 20 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
CHEMBL412939 161032 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1604 53 23 20 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
1679 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44143437 178049 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL467533 178049 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
16131448 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44143433 177981 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL467057 177981 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143433 177981 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467057 177981 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL269029 209020 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
16131448 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
45273531 193242 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL541511 193242 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL504461 212397 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
72548703 161007 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysisDisplacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161007 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysisDisplacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
44143451 178128 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468315 178128 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL505873 212418 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL525604 213871 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1679 266 21 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
9963005 266 21 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL437723 266 21 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44143456 178010 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467279 178010 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44576628 187134 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL495402 187134 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
44143430 188788 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL512975 188788 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL504540 212399 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL524339 213818 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL524873 213840 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
24857820 96224 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263918 96224 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
24857820 96224 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL263918 96224 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL389521 210670 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2016.11.014
16131448 2796 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
1681 2796 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
1688 2796 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
44361543 2796 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
56947112 2796 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
CHEMBL396460 2796 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
118717442 114621 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 953 31 16 12 -1.6 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2014.09.018
CHEMBL3343948 114621 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 953 31 16 12 -1.6 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2014.09.018
9823363 177882 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466308 177882 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
45273546 194092 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557721 194092 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143450 188220 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL506207 188220 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45269358 194507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561397 194507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
16131448 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1681 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1688 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44361543 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
56947112 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL396460 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL526352 213896 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
101354795 114622 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343949 114622 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
44143455 177875 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466252 177875 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44456220 154888 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL403807 154888 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
16131448 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1681 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1688 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44361543 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
56947112 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL396460 2796 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44450085 96223 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263917 96223 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
44143457 178011 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467280 178011 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
16131448 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44456185 166057 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL428076 166057 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44143448 178071 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467677 178071 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44189735 13894 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197249 13894 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563980 13894 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
11619553 161159 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
CHEMBL413571 161159 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
22272974 96217 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263903 96217 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
15982795 71792 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 4 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(CC3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL197942 71792 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 4 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(CC3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44404679 167859 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL434944 167859 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44406497 135472 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL373170 135472 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
44406604 140077 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 419 3 2 4 3.6 Cc1ccccc1[C@]1(O)CCCC[C@H]1N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2005.09.067
CHEMBL381419 140077 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 419 3 2 4 3.6 Cc1ccccc1[C@]1(O)CCCC[C@H]1N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2005.09.067
44406603 165499 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 2 4 3.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL425753 165499 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 2 4 3.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
15982659 71940 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 440 5 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198322 71940 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 440 5 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44404706 134667 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 378 4 0 4 3.3 COC(=O)CN1C(=O)C2(CCN(C(C)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL372135 134667 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 378 4 0 4 3.3 COC(=O)CN1C(=O)C2(CCN(C(C)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
15983065 134825 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 5 4.5 COC(=O)CN1C(=O)C2(CCN(Cc3ccccc3-c3ccsc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL372779 134825 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 5 4.5 COC(=O)CN1C(=O)C2(CCN(Cc3ccccc3-c3ccsc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
15982796 140349 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 442 12 0 4 5.3 CCCCCCC(CCCC)CN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
CHEMBL382086 140349 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 442 12 0 4 5.3 CCCCCCC(CCCC)CN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
44406587 72487 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 473 3 2 4 4.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)c(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200227 72487 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 473 3 2 4 4.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)c(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
44406503 168074 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 2 4 3.5 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL436295 168074 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 2 4 3.5 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
44406543 134723 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 457 3 2 4 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL372567 134723 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 457 3 2 4 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
44404711 132479 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 404 3 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL370226 132479 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 404 3 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44143418 186646 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL492585 186646 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
45271041 194700 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 331 5 1 3 5.1 Cc1nc(CNC2CCCC2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL562663 194700 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 331 5 1 3 5.1 Cc1nc(CNC2CCCC2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL404792 210776 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
52915518 60238 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 511 13 4 6 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1760025 60238 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 511 13 4 6 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915270 60595 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 468 10 3 5 5.8 CCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762398 60595 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 468 10 3 5 5.8 CCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
15982938 132982 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 454 4 0 4 5.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL370782 132982 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 454 4 0 4 5.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
52916471 60575 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 930 21 4 10 12.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762378 60575 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 930 21 4 10 12.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916266 60609 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 6 3 5 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762412 60609 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 6 3 5 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
11633324 72318 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
CHEMBL199639 72318 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
11619363 74074 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 452 7 1 3 5.0 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(=O)c1ccccc1 10.1021/jm0509851
CHEMBL202715 74074 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 452 7 1 3 5.0 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(=O)c1ccccc1 10.1021/jm0509851
45273547 194113 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 365 6 1 4 3.7 CC(=O)Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557925 194113 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 365 6 1 4 3.7 CC(=O)Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
15982661 132908 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 512 9 2 6 3.0 O=C1N(CC(O)CNCCN2CCOCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL370613 132908 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 512 9 2 6 3.0 O=C1N(CC(O)CNCCN2CCOCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44404670 134671 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 416 4 0 2 5.9 O=C1N(Cc2ccccc2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL372184 134671 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 416 4 0 2 5.9 O=C1N(Cc2ccccc2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
22273116 96218 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 354 5 2 5 2.8 CC(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263904 96218 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 354 5 2 5 2.8 CC(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
136043786 77004 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 421 5 1 5 4.4 CN1CCN(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL208602 77004 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 421 5 1 5 4.4 CN1CCN(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
52915390 60597 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 496 12 3 5 6.6 CCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762400 60597 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 496 12 3 5 6.6 CCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL405948 210830 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
44143422 186932 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1cncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)c1 10.1016/j.bmcl.2009.04.116
CHEMBL494406 186932 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1cncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)c1 10.1016/j.bmcl.2009.04.116
CHEMBL526142 213887 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
45273662 194167 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2cc(CNC3CCCC3)nn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL558524 194167 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2cc(CNC3CCCC3)nn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
44406621 72532 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200371 72532 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
44407084 139817 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 477 7 1 5 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COCN1C(=O)OCc1ccccc1 10.1021/jm0509851
CHEMBL380786 139817 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 477 7 1 5 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COCN1C(=O)OCc1ccccc1 10.1021/jm0509851
44404653 140764 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 3 5.9 COc1ccc(CN2C(=O)C3(CCN(CC4CCCCCCC4)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.08.009
CHEMBL383371 140764 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 3 5.9 COc1ccc(CN2C(=O)C3(CCN(CC4CCCCCCC4)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.08.009
44406557 72614 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccnc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200695 72614 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccnc1)CC2 10.1016/j.bmcl.2005.09.067
118726267 116719 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394749 116719 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
44456187 95184 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL257921 95184 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44456412 97022 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270231 97022 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
15982658 96238 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3cccc(C(F)(F)F)c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL264066 96238 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3cccc(C(F)(F)F)c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44449771 155098 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 342 4 2 4 3.4 Fc1cc2nc(SCc3ccccc3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL404771 155098 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 342 4 2 4 3.4 Fc1cc2nc(SCc3ccccc3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
136043771 77809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 366 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210504 77809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 366 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
52915147 60590 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 508 12 2 5 7.3 CCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762393 60590 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 508 12 2 5 7.3 CCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915635 60606 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 539 15 4 6 6.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762409 60606 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 539 15 4 6 6.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915266 60591 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 522 13 2 5 7.7 CCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762394 60591 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 522 13 2 5 7.7 CCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44450151 95335 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258711 95335 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45270917 193363 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL549439 193363 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
45270928 193905 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 2 4 3.1 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCO)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL555354 193905 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 2 4 3.1 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCO)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
24847114 154835 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
CHEMBL403515 154835 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
44404695 72138 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
CHEMBL199011 72138 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
44143408 177953 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 7 1 3 6.9 Cc1c(CNCCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL466843 177953 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 7 1 3 6.9 Cc1c(CNCCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44143407 192605 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 421 6 1 3 6.6 Cc1c(CNCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL523530 192605 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 421 6 1 3 6.6 Cc1c(CNCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44406538 72480 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200204 72480 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
44406551 133293 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccn1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL371550 133293 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccn1)CC2 10.1016/j.bmcl.2005.09.067
18441735 79086 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1(O)c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
CHEMBL211373 79086 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1(O)c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
52915637 60608 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 567 17 4 6 7.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762411 60608 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 567 17 4 6 7.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915267 60592 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 536 14 2 5 8.1 CCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762395 60592 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 536 14 2 5 8.1 CCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915515 60602 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 469 10 4 6 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762405 60602 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 469 10 4 6 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44574053 178036 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467473 178036 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44456299 97017 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270216 97017 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
118726265 116717 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
CHEMBL3394747 116717 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
45271902 193843 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 465 7 1 3 7.2 FCCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL554058 193843 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 465 7 1 3 7.2 FCCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
45269372 194976 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 489 8 1 3 8.6 CCC(CC)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL564484 194976 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 489 8 1 3 8.6 CCC(CC)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
45268503 195017 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 447 6 1 3 7.2 CCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL564837 195017 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 447 6 1 3 7.2 CCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
118726264 116716 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394746 116716 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
22272877 95439 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259185 95439 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
22272900 96213 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263889 96213 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
45268356 194853 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 339 4 1 3 4.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(Cl)c1 10.1016/j.bmcl.2009.06.051
CHEMBL563686 194853 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 339 4 1 3 4.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(Cl)c1 10.1016/j.bmcl.2009.06.051
22272877 95439 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL259185 95439 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44407070 73566 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 394 7 1 3 4.3 O=C(CSc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202059 73566 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 394 7 1 3 4.3 O=C(CSc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
118726273 116726 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 649 11 2 6 5.3 Cc1ccc(CN(C[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)C(=O)[C@H](N)C(C)C)cc1 10.1016/j.bmcl.2014.12.015
CHEMBL3394756 116726 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 649 11 2 6 5.3 Cc1ccc(CN(C[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)C(=O)[C@H](N)C(C)C)cc1 10.1016/j.bmcl.2014.12.015
44576627 192629 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL523724 192629 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44404731 135505 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 412 5 0 4 4.3 CC(=O)OCCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL373190 135505 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 412 5 0 4 4.3 CC(=O)OCCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44449767 95563 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1cccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)c1 10.1016/j.bmcl.2008.04.054
CHEMBL259764 95563 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1cccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)c1 10.1016/j.bmcl.2008.04.054
52915268 60593 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 550 15 2 5 8.5 CCCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762396 60593 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 550 15 2 5 8.5 CCCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915145 60588 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 480 10 2 5 6.6 CCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762391 60588 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 480 10 2 5 6.6 CCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
10004950 9939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 470 5 1 6 2.5 CNC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
CHEMBL115222 9939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 470 5 1 6 2.5 CNC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
45271885 194939 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 459 6 1 3 7.5 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CC2)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL564225 194939 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 459 6 1 3 7.5 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CC2)cc1 10.1016/j.bmcl.2009.06.095
44342270 9822 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 9822 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
44143435 177857 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466112 177857 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
45270907 194076 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557623 194076 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
22273044 95334 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258710 95334 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143449 178006 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467266 178006 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL510117 213795 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL510117 213795 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
1681 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
1688 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
44361543 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
56947112 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
CHEMBL396460 2796 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
24882570 114620 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 114620 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 114620 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
44143453 177896 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466448 177896 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL455289 212239 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1691 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
5311194 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
CHEMBL357076 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
1691 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
5311194 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
CHEMBL357076 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
44189834 13893 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197240 13893 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563657 13893 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44189733 13901 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197275 13901 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL564840 13901 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
1691 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
5311194 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
CHEMBL357076 2067 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
44143432 178123 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL468302 178123 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143432 178123 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468302 178123 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143428 178126 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468308 178126 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
24857819 186924 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
24857819 186924 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL494350 186924 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL494350 186924 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44456140 168138 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL436852 168138 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44450086 157738 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
CHEMBL408901 157738 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
416359 101377 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]-Tyr14 at nociceptin (NOP) receptorAbility to displace [125I]-Tyr14 at nociceptin (NOP) receptor
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.09.068
CHEMBL300616 101377 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]-Tyr14 at nociceptin (NOP) receptorAbility to displace [125I]-Tyr14 at nociceptin (NOP) receptor
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.09.068
416359 101377 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
CHEMBL300616 101377 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
45267616 194603 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 432 5 1 2 7.4 Cc1c(CNC2CCCC2)cc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL562077 194603 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 432 5 1 2 7.4 Cc1c(CNC2CCCC2)cc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
52915517 60604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 497 12 4 6 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762407 60604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 497 12 4 6 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916174 60610 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 5 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C=O)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762413 60610 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 5 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C=O)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915146 60589 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 494 11 2 5 7.0 CCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762392 60589 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 494 11 2 5 7.0 CCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44407116 73839 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 438 7 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Cc1ccccc1 10.1021/jm0509851
CHEMBL202322 73839 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 438 7 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Cc1ccccc1 10.1021/jm0509851
44143445 177870 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466221 177870 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44455999 97049 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL270394 97049 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44456339 168316 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 34 15 11 -0.1 CCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL438383 168316 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 34 15 11 -0.1 CCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
45269228 194247 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 373 4 1 3 4.5 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL559402 194247 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 373 4 1 3 4.5 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.051
136043790 77692 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CN(C)CCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210000 77692 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CN(C)CCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
52915636 60607 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 16 4 6 6.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762410 60607 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 16 4 6 6.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL444110 212170 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44143444 177842 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 352 3 1 4 4.2 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466020 177842 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 352 3 1 4 4.2 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
579 3083 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
6918468 3083 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
CHEMBL41547 3083 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
11710187 71721 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 2 0 2 4.5 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2005.08.009
CHEMBL197727 71721 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 2 0 2 4.5 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2005.08.009
44450209 95757 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260821 95757 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44143439 172171 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 402 4 1 4 4.9 C[C@@H]1CN(CC(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL450887 172171 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 402 4 1 4 4.9 C[C@@H]1CN(CC(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44407085 73682 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 439 7 2 3 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Nc1ccccc1 10.1021/jm0509851
CHEMBL202220 73682 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 439 7 2 3 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Nc1ccccc1 10.1021/jm0509851
136043796 78595 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 374 7 1 4 4.4 Cc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
CHEMBL211310 78595 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 374 7 1 4 4.4 Cc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
44407133 74037 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 1 4 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COC(=O)N1Cc1ccccc1 10.1021/jm0509851
CHEMBL202492 74037 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 1 4 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COC(=O)N1Cc1ccccc1 10.1021/jm0509851
44450180 156210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 442 4 2 5 3.4 O=S(=O)(Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407068 156210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 442 4 2 5 3.4 O=S(=O)(Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44404684 140085 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 3 0 3 4.4 COc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
CHEMBL381429 140085 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 3 0 3 4.4 COc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
11811722 9955 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
CHEMBL115280 9955 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
52915634 60605 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 525 14 4 6 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762408 60605 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 525 14 4 6 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
11411841 60568 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 835 16 0 6 10.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN2CN(c4ccccc4)C4(CCN([C@H]5CC[C@@H](C(C)C)CC5)CC4)C2=O)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
CHEMBL1762371 60568 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 835 16 0 6 10.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN2CN(c4ccccc4)C4(CCN([C@H]5CC[C@@H](C(C)C)CC5)CC4)C2=O)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
15982935 169696 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL444620 169696 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
118726268 116720 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394750 116720 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
45271015 193855 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 381 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL554299 193855 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 381 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C)cn1 10.1016/j.bmcl.2009.06.095
44404689 167744 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 356 2 1 3 4.1 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(O)cc21 10.1016/j.bmcl.2005.08.009
CHEMBL434179 167744 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 356 2 1 3 4.1 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(O)cc21 10.1016/j.bmcl.2005.08.009
9823363 188654 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL511742 188654 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143442 177917 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL466630 177917 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44143421 186907 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 5 1 5 5.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL494231 186907 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 5 1 5 5.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL268145 208985 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
15983067 72170 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 3 4.8 CCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(OC)cc21 10.1016/j.bmcl.2005.08.009
CHEMBL199095 72170 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 3 4.8 CCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(OC)cc21 10.1016/j.bmcl.2005.08.009
44143413 188772 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL512827 188772 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44143413 188772 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL512827 188772 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
45267601 194414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL560875 194414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
52915031 60584 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 949 24 6 10 11.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762387 60584 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 949 24 6 10 11.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
10949380 163460 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 6 4.3 Cc1ccc2nc(O)n(C3CCN(Cc4cc5c(cc4Cl)OCO5)CC3)c2c1 10.1021/jm010878g
CHEMBL420863 163460 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 6 4.3 Cc1ccc2nc(O)n(C3CCN(Cc4cc5c(cc4Cl)OCO5)CC3)c2c1 10.1021/jm010878g
44404646 139753 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 1 3 3.7 O=C1N(CCO)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL380603 139753 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 1 3 3.7 O=C1N(CCO)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44407086 73308 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 451 7 1 5 4.9 O=C(CSc1nc2ccccc2s1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL201826 73308 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 451 7 1 5 4.9 O=C(CSc1nc2ccccc2s1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
44449793 157105 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 266 2 2 4 1.8 CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL408148 157105 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 266 2 2 4 1.8 CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44450207 158894 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 426 4 2 4 3.7 [O-][S+](Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL410124 158894 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 426 4 2 4 3.7 [O-][S+](Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL442113 212149 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL435511 211909 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
45273537 194744 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL562932 194744 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
45268498 195016 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
CHEMBL564812 195016 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
44456141 94897 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL256687 94897 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
118726269 116721 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 654 14 2 8 5.3 COc1ccc(CCNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
CHEMBL3394751 116721 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 654 14 2 8 5.3 COc1ccc(CCNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
44407044 140034 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 2 4 3.2 O=C1N[C@@H](Cc2ccccc2)[C@@H](C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)O1 10.1021/jm0509851
CHEMBL381287 140034 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 2 4 3.2 O=C1N[C@@H](Cc2ccccc2)[C@@H](C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)O1 10.1021/jm0509851
1692 2114 23 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
5311340 2114 23 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
CHEMBL140979 2114 23 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
52916714 60582 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 920 22 6 10 11.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762385 60582 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 920 22 6 10 11.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44406618 133063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL371267 133063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
52915393 60600 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 538 15 3 5 7.8 CCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762403 60600 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 538 15 3 5 7.8 CCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915144 60587 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 466 9 2 5 6.2 CCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762390 60587 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 466 9 2 5 6.2 CCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44449764 156698 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
CHEMBL407653 156698 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
52915030 60583 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 934 23 6 10 11.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762386 60583 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 934 23 6 10 11.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44406618 133063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL371267 133063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
22273255 156969 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 346 6 2 5 3.5 CCC(CC)Sc1nc2cc(C(C)=O)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407991 156969 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 346 6 2 5 3.5 CCC(CC)Sc1nc2cc(C(C)=O)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
11544654 69911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 340 2 0 2 4.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL194200 69911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 340 2 0 2 4.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
52915032 60585 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 963 25 6 10 12.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762388 60585 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 963 25 6 10 12.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
15982791 72014 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 531 9 1 4 5.9 CCN(Cc1ccc(C)cc1)CC(O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198604 72014 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 531 9 1 4 5.9 CCN(Cc1ccc(C)cc1)CC(O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
17858339 96212 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 304 5 2 4 3.3 CCC(CC)Sc1nc2ccc(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263888 96212 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 304 5 2 4 3.3 CCC(CC)Sc1nc2ccc(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45267506 194378 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 415 7 1 5 3.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCS(C)(=O)=O)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560469 194378 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 415 7 1 5 3.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCS(C)(=O)=O)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143423 186936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 361 5 1 5 4.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494413 186936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 361 5 1 5 4.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C)cn1 10.1016/j.bmcl.2009.04.116
45268504 194427 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 461 6 1 3 7.8 CC(C)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL560937 194427 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 461 6 1 3 7.8 CC(C)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44407140 74051 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 6 2 3 3.8 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C(=O)c1c[nH]c2ccccc12 10.1021/jm0509851
CHEMBL202604 74051 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 6 2 3 3.8 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C(=O)c1c[nH]c2ccccc12 10.1021/jm0509851
23542099 116712 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 592 12 1 5 6.3 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccc(F)cc2)C2(CCN(CC3CCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394742 116712 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 592 12 1 5 6.3 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccc(F)cc2)C2(CCN(CC3CCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
44407112 73575 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.5 O=C(Cc1cccc(Oc2ccccc2)c1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202091 73575 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.5 O=C(Cc1cccc(Oc2ccccc2)c1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
10948527 110854 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
CHEMBL326962 110854 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
52916358 60571 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 874 17 4 10 10.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762374 60571 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 874 17 4 10 10.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44404721 71834 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 3 0 4 4.0 COC(=O)CN1C(=O)C2(CCN(c3ccc4c5c(cccc35)CC4)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198046 71834 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 3 0 4 4.0 COC(=O)CN1C(=O)C2(CCN(c3ccc4c5c(cccc35)CC4)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
11523972 165600 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 390 8 1 2 4.5 O=C(CCCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL426303 165600 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 390 8 1 2 4.5 O=C(CCCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
44143406 186906 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL494230 186906 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44143424 192114 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.0 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C(F)(F)F)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL522021 192114 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.0 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C(F)(F)F)cn1 10.1016/j.bmcl.2009.04.116
44407048 73576 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 7 2 2 4.6 O=C(CCc1c[nH]c2ccccc12)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202094 73576 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 7 2 2 4.6 O=C(CCc1c[nH]c2ccccc12)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
15983063 140797 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 328 4 0 4 2.0 COC(=O)CN1C(=O)C2(CCN(CC3CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL383561 140797 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 328 4 0 4 2.0 COC(=O)CN1C(=O)C2(CCN(CC3CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44404699 168214 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1cccc2c1C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
CHEMBL437505 168214 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1cccc2c1C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
118726272 116724 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 8 1 5 6.1 Cc1cccc(SC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)c1 10.1016/j.bmcl.2014.12.015
CHEMBL3394754 116724 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 8 1 5 6.1 Cc1cccc(SC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)c1 10.1016/j.bmcl.2014.12.015
44143415 178199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL468937 178199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL384866 210582 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
11406629 140794 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL383539 140794 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
44574003 177918 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL466631 177918 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
10937901 9802 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1021/jm010878g
CHEMBL114379 9802 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1021/jm010878g
44404652 72216 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 326 2 1 2 4.3 O=C1Nc2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL199248 72216 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 326 2 1 2 4.3 O=C1Nc2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44406540 72649 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200882 72649 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL406010 210834 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H]1NC(=O)CNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
44143419 187012 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494767 187012 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
118726262 116714 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
CHEMBL3394744 116714 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
45268355 194556 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL561732 194556 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
44143446 177871 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466222 177871 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
10763594 160718 1 None 120 4 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1016/j.ejmech.2011.01.040
CHEMBL412098 160718 1 None 120 4 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1016/j.ejmech.2011.01.040
17858448 95499 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259452 95499 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45269357 194506 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561396 194506 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL424934 211569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
135458466 79097 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL211390 79097 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
118726270 116722 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 546 9 2 6 4.8 CC(C)(C)NC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394752 116722 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 546 9 2 6 4.8 CC(C)(C)NC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
44406719 165532 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 1 3 4.8 O=C1NCN(c2ccc(Cl)cc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL425929 165532 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 1 3 4.8 O=C1NCN(c2ccc(Cl)cc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
52915514 60601 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 552 16 3 5 8.2 CCCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762404 60601 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 552 16 3 5 8.2 CCCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
136043824 79506 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 396 7 1 5 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(COc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL212520 79506 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 396 7 1 5 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(COc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
10905740 110168 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL325945 110168 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
136043756 77965 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.7 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CC5CCC4C5)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211053 77965 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.7 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CC5CCC4C5)no3)cc12 10.1016/j.bmcl.2006.03.086
136043767 79307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 6 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211617 79307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 6 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
44456216 154849 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL403588 154849 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44404698 132207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
CHEMBL369945 132207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
136043795 77715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210140 77715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
136043817 79415 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(Cc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL212161 79415 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(Cc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11525624 133003 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL370870 133003 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
44456298 168227 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL437601 168227 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44404694 72037 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198678 72037 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
52916267 60570 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 860 16 4 10 10.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762373 60570 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 860 16 4 10 10.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915392 60599 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 14 3 5 7.4 CCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762402 60599 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 14 3 5 7.4 CCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
136043800 77422 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209213 77422 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
155533462 171257 0 None 15 2 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assayAntagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assay
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4468676 171257 0 None 15 2 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assayAntagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assay
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
11191683 60569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 13 0 4 6.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN(C)C)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
CHEMBL1762372 60569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 13 0 4 6.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN(C)C)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
10199945 96225 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263919 96225 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44456101 97372 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 33 15 11 -0.5 CCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL272084 97372 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 33 15 11 -0.5 CCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44143434 177931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466702 177931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
10832076 37803 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
CHEMBL146054 37803 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
44407129 73665 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 445 7 1 3 3.7 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCC(=O)N1Cc1ccccc1 10.1021/jm0509851
CHEMBL202204 73665 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 445 7 1 3 3.7 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCC(=O)N1Cc1ccccc1 10.1021/jm0509851
52916359 60572 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 888 18 4 10 10.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762375 60572 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 888 18 4 10 10.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
45270203 194766 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 483 7 1 3 7.5 FC(F)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL563073 194766 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 483 7 1 3 7.5 FC(F)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
15982524 165718 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 4 3.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL427010 165718 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 4 3.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
45271862 193449 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL550117 193449 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44143414 178198 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccccn1 10.1016/j.bmcl.2009.04.116
CHEMBL468936 178198 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccccn1 10.1016/j.bmcl.2009.04.116
45270196 193714 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 473 6 1 3 7.9 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CCC2)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL552011 193714 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 473 6 1 3 7.9 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CCC2)cc1 10.1016/j.bmcl.2009.06.095
11559820 165407 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 374 6 1 2 4.2 O=C(/C=C/c1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL425225 165407 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 374 6 1 2 4.2 O=C(/C=C/c1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
45270202 193770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 475 7 1 3 7.9 CC(C)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL552417 193770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 475 7 1 3 7.9 CC(C)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44450210 95758 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260822 95758 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
52916599 60579 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 878 19 6 10 9.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762382 60579 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 878 19 6 10 9.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44143412 177873 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 4 0 3 6.8 Cc1c(CN2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL466226 177873 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 4 0 3 6.8 Cc1c(CN2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
136043797 77126 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 390 8 1 5 4.1 COc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
CHEMBL208725 77126 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 390 8 1 5 4.1 COc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
136043781 77631 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 7 1 4 5.3 Clc1ccc(CCc2noc(-c3cc4c(CCN5CCCC5)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
CHEMBL209728 77631 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 7 1 4 5.3 Clc1ccc(CCc2noc(-c3cc4c(CCN5CCCC5)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
136043779 77744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210292 77744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11676849 73154 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 7 2 3 4.9 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(O)c1ccccc1 10.1021/jm0509851
CHEMBL201694 73154 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 7 2 3 4.9 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(O)c1ccccc1 10.1021/jm0509851
136043765 79302 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 7 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211592 79302 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 7 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
44406550 135516 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1cccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)c1 10.1016/j.bmcl.2005.09.067
CHEMBL373198 135516 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1cccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)c1 10.1016/j.bmcl.2005.09.067
44450208 95756 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260820 95756 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
45270082 193565 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL551002 193565 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
10451761 37753 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
CHEMBL146013 37753 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
10783436 37952 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
CHEMBL146191 37952 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
44143452 178150 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468524 178150 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
15982530 72013 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 408 2 0 2 5.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198600 72013 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 408 2 0 2 5.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2005.08.009
136043792 77005 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3noc(CCc4ccc(Cl)cc4)n3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL208603 77005 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3noc(CCc4ccc(Cl)cc4)n3)cc12 10.1016/j.bmcl.2006.03.086
44406489 140808 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
44406489 140808 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
44406489 140808 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.064
CHEMBL383610 140808 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL383610 140808 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL383610 140808 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.064
15965865 137822 4 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
CHEMBL377140 137822 4 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
118726261 116713 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
CHEMBL3394743 116713 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
44143441 177889 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 377 3 1 5 4.1 C[C@@H]1CN(CC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL466427 177889 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 377 3 1 5 4.1 C[C@@H]1CN(CC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44143417 186621 7 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 367 5 1 5 4.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL492396 186621 7 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 367 5 1 5 4.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
11372671 137826 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 388 3 1 2 4.8 O=C1NCC(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
CHEMBL377164 137826 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 388 3 1 2 4.8 O=C1NCC(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
136043782 138122 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL377736 138122 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
136043788 138800 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL379284 138800 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
45270174 193517 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2nc(CNC3CCCC3)cn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL550601 193517 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2nc(CNC3CCCC3)cn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
44449822 95411 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 360 4 2 4 3.5 Fc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
CHEMBL259065 95411 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 360 4 2 4 3.5 Fc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
52916470 60574 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 916 20 4 10 11.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762377 60574 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 916 20 4 10 11.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44407013 74045 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 430 6 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C1(c2ccccc2)CCCCC1 10.1021/jm0509851
CHEMBL202575 74045 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 430 6 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C1(c2ccccc2)CCCCC1 10.1021/jm0509851
44143440 178069 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 420 3 1 4 5.2 C[C@@H]1CN(CC(F)(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL467669 178069 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 420 3 1 4 5.2 C[C@@H]1CN(CC(F)(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
52915391 60598 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 510 13 3 5 7.0 CCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762401 60598 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 510 13 3 5 7.0 CCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44143420 187013 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 395 6 1 5 4.9 CCc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494768 187013 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 395 6 1 5 4.9 CCc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
15982526 71724 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 422 4 0 2 6.3 O=C1N(CC2CCCCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL197735 71724 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 422 4 0 2 6.3 O=C1N(CC2CCCCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44143427 188886 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL513855 188886 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44143454 188576 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL511205 188576 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44456028 155047 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL404530 155047 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44517710 194838 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL563593 194838 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44406539 134639 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1ccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)cc1 10.1016/j.bmcl.2005.09.067
CHEMBL371966 134639 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1ccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)cc1 10.1016/j.bmcl.2005.09.067
136043759 78284 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211254 78284 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
52916713 60581 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 906 21 6 10 10.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762384 60581 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 906 21 6 10 10.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44404693 135557 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL373222 135557 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44143425 186937 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 425 6 1 7 3.4 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2S(C)(=O)=O)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494414 186937 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 425 6 1 7 3.4 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2S(C)(=O)=O)cn1 10.1016/j.bmcl.2009.04.116
44576626 192753 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL525054 192753 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
11603249 72828 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 376 7 1 2 4.1 O=C(CCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL201181 72828 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 376 7 1 2 4.1 O=C(CCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
52915389 60596 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 482 11 3 5 6.2 CCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762399 60596 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 482 11 3 5 6.2 CCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
15982529 71783 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 3 0 2 5.5 CC(C)c1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
CHEMBL197895 71783 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 3 0 2 5.5 CC(C)c1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
44143409 177980 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 447 5 1 3 7.2 Cc1c(CNC2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL467049 177980 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 447 5 1 3 7.2 Cc1c(CNC2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
10981761 110136 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
CHEMBL325750 110136 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
52916712 60580 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 892 20 6 10 10.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762383 60580 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 892 20 6 10 10.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916598 60578 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 864 18 6 10 9.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762381 60578 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 864 18 6 10 9.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44449766 155143 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL405078 155143 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
52915516 60603 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 483 11 4 6 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762406 60603 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 483 11 4 6 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
118726266 116718 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
CHEMBL3394748 116718 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
44576625 186905 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL494219 186905 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
11583016 73989 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
CHEMBL202443 73989 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
44178080 194396 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560667 194396 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143426 178125 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncc(Cl)cc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468307 178125 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncc(Cl)cc2Cl)cn1 10.1016/j.bmcl.2009.04.116
24882570 114620 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 114620 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 114620 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
45273679 193952 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
CHEMBL556300 193952 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
CHEMBL266667 208938 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
118726271 116723 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 4.8 COc1ccc(CCNC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
CHEMBL3394753 116723 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 4.8 COc1ccc(CCNC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
15983062 71855 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198099 71855 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
23542106 116725 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 611 12 1 7 5.3 COc1ccc(CCOC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
CHEMBL3394755 116725 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 611 12 1 7 5.3 COc1ccc(CCOC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
52916597 60577 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 958 23 4 10 12.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762380 60577 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 958 23 4 10 12.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916472 60576 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 944 22 4 10 12.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762379 60576 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 944 22 4 10 12.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
15982797 71881 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 7 0 4 3.1 CCCCCCN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
CHEMBL198167 71881 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 7 0 4 3.1 CCCCCCN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
9887195 38292 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 CCn1c(=O)n([C@H]2CCN(CC3CCCCCCC3)C[C@@H]2CO)c2ccccc21 10.1021/jm990517p
CHEMBL146462 38292 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 CCn1c(=O)n([C@H]2CCN(CC3CCCCCCC3)C[C@@H]2CO)c2ccccc21 10.1021/jm990517p
44449850 160682 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 450 6 1 4 5.5 Fc1ccc(CSc2nc3cc(F)c(N4CCN(Cc5ccccc5)CC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
CHEMBL411890 160682 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 450 6 1 4 5.5 Fc1ccc(CSc2nc3cc(F)c(N4CCN(Cc5ccccc5)CC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
15982660 72096 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 4 0 3 4.1 O=C1N(CC2CO2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL198867 72096 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 4 0 3 4.1 O=C1N(CC2CO2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
11597677 73299 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
CHEMBL201805 73299 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
52915269 60594 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 454 9 3 5 5.5 CCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762397 60594 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 454 9 3 5 5.5 CCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52916360 60573 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 902 19 4 10 11.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762376 60573 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 902 19 4 10 11.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
45271014 193779 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2)c1-c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2009.06.095
CHEMBL552482 193779 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2)c1-c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2009.06.095
44407020 73603 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.0 CC(C)(Oc1ccc(Cl)cc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202152 73603 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.0 CC(C)(Oc1ccc(Cl)cc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL405451 210805 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
15982657 71781 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL197880 71781 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
45270184 193590 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL551208 193590 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
44143438 178146 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL468504 178146 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
45267505 194377 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560468 194377 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143429 178149 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468518 178149 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44143432 178122 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468301 178122 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
10221539 156444 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407325 156444 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
10221539 156444 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL407325 156444 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44143436 177881 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466307 177881 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
45272626 194081 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL557653 194081 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
15982937 139734 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 410 3 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL380580 139734 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 410 3 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44407156 140785 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 1 3 3.9 CC(Oc1ccccc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL383489 140785 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 1 3 3.9 CC(Oc1ccccc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
44449851 95337 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 374 4 1 4 3.9 CN1CCN(c2cc3[nH]c(SCc4ccc(F)cc4)nc3cc2F)CC1 10.1016/j.bmcl.2008.04.054
CHEMBL258746 95337 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 374 4 1 4 3.9 CN1CCN(c2cc3[nH]c(SCc4ccc(F)cc4)nc3cc2F)CC1 10.1016/j.bmcl.2008.04.054
44456217 169102 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCC(CC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL443765 169102 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCC(CC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
136043819 77568 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209537 77568 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
45273702 194094 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 497 8 1 3 7.7 FCC(CF)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL557729 194094 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 497 8 1 3 7.7 FCC(CF)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
136043780 138725 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL379048 138725 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11143820 10012 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 5 3.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cc3c(cc1Cl)OCO3)CC2 10.1021/jm010878g
CHEMBL115652 10012 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 5 3.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cc3c(cc1Cl)OCO3)CC2 10.1021/jm010878g
52915143 60586 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 452 8 2 5 5.8 CCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762389 60586 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 452 8 2 5 5.8 CCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
118726263 116715 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394745 116715 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
16131448 2796 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1681 2796 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1688 2796 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
44361543 2796 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
56947112 2796 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
CHEMBL396460 2796 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
16131448 2796 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2796 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2796 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2796 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2796 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2796 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
16131448 2796 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
24882570 114620 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 114620 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 114620 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
101232765 179234 0 None - 1 Human 7.0 pKd = 7.0 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4745049 179234 0 None - 1 Human 7.0 pKd = 7.0 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657543 180543 0 None - 1 Human 7.9 pKd = 7.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760649 180543 0 None - 1 Human 7.9 pKd = 7.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
101232765 179234 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4745049 179234 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410396 211061 16 None 1 2 Human 7.8 pKd = 7.8 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657543 180543 0 None - 1 Human 7.7 pKd = 7.7 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760649 180543 0 None - 1 Human 7.7 pKd = 7.7 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10654047 210873 16 None 2 2 Human 7.5 pKd = 7.5 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406946 210873 16 None 2 2 Human 7.5 pKd = 7.5 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410396 211061 16 None 1 2 Human 8.2 pKd = 8.2 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10654047 210873 16 None 2 2 Human 7.1 pKd = 7.1 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406946 210873 16 None 2 2 Human 7.1 pKd = 7.1 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
44388467 168828 0 None - 1 Human 10.7 pKi = 10.7 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 168828 0 None - 1 Human 10.7 pKi = 10.7 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL415845 211446 0 None - 1 Human 10.7 pKi = 10.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL264846 208877 0 None - 1 Human 10.7 pKi = 10.7 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388474 160483 0 None - 1 Human 10.6 pKi = 10.6 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL411649 160483 0 None - 1 Human 10.6 pKi = 10.6 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
3917 3855 0 None 154 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None 154 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None 154 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1641 2678 6 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
3829 2678 6 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
5497186 2678 6 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
CHEMBL567175 2678 6 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
44388466 96041 0 None - 1 Human 10.5 pKi = 10.5 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 96041 0 None - 1 Human 10.5 pKi = 10.5 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
70689062 77234 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 438 5 1 4 4.3 NC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088054 77234 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 438 5 1 4 4.3 NC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL3810319 210520 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL263588 208824 0 None - 1 Human 10.3 pKi = 10.3 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
16131448 2796 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
1681 2796 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
1688 2796 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
44361543 2796 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
56947112 2796 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2796 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
CHEMBL266191 208924 0 None - 1 Human 10.3 pKi = 10.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL414542 211380 0 None - 1 Human 10.3 pKi = 10.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL3808650 210517 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL2372052 208419 0 None 5 7 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL438537 212016 0 None - 1 Human 10.2 pKi = 10.2 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
16131448 2796 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
1681 2796 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
1688 2796 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
44361543 2796 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
56947112 2796 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
CHEMBL396460 2796 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
68182754 112179 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 472 5 0 6 4.6 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236476 112179 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 472 5 0 6 4.6 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304248 112179 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 472 5 0 6 4.6 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
70684842 77239 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 460 6 0 4 4.4 CN(C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
CHEMBL2088061 77239 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 460 6 0 4 4.4 CN(C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
68182860 112193 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 3 0 5 4.7 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236474 112193 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 3 0 5 4.7 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304364 112193 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 3 0 5 4.7 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
9885005 57228 0 None 40 4 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL166387 57228 0 None 40 4 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL408356 210951 0 None - 1 Human 10.1 pKi = 10.1 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
16131448 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1681 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1688 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
44361543 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
56947112 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL396460 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
9842289 119964 0 None 8 4 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354291 119964 0 None 8 4 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
12419 2429 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 2429 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 2429 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
58268629 77907 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088055 77907 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2109704 77907 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
52951809 83168 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204347 83168 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
70684841 77237 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088058 77237 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
58268628 112141 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 0 7 4.5 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236478 112141 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 0 7 4.5 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3303098 112141 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 0 7 4.5 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
58268566 109618 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 516 4 1 7 5.3 Cc1nn(-c2ncccc2-c2ncc[nH]2)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236486 109618 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 516 4 1 7 5.3 Cc1nn(-c2ncccc2-c2ncc[nH]2)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
58268647 112105 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 0 7 4.0 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(F)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236479 112105 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 0 7 4.0 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(F)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3302393 112105 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 0 7 4.0 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(F)sc23)c(C)n1 10.1021/jm500117r
68182857 112185 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 4 1 6 3.7 Cc1nn(-c2c(F)cccc2C(N)=O)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236475 112185 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 4 1 6 3.7 Cc1nn(-c2c(F)cccc2C(N)=O)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304315 112185 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 4 1 6 3.7 Cc1nn(-c2c(F)cccc2C(N)=O)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
67168385 112191 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 5 1 6 5.4 CNCc1cccc(F)c1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236485 112191 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 5 1 6 5.4 CNCc1cccc(F)c1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3304360 112191 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 5 1 6 5.4 CNCc1cccc(F)c1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL264084 208850 0 None - 1 Human 10.0 pKi = 10 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
16131448 2796 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
1681 2796 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
1688 2796 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
44361543 2796 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
56947112 2796 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 2796 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
CHEMBL1162359 206765 0 None - 1 Human 10.0 pKi = 10 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
25208097 183330 3 None 5 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481366 183330 3 None 5 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
10406239 120036 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326224 120036 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326226 120036 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545624 120036 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
52951675 83171 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204353 83171 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
52914971 2365 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
9462 2365 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
CHEMBL3304244 2365 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
DB16048 2365 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
52951807 77012 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2086410 77012 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951807 77012 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2086410 77012 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
68182737 112107 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 4 1 6 5.1 Cc1nn(-c2c(F)cccc2CO)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236484 112107 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 4 1 6 5.1 Cc1nn(-c2c(F)cccc2CO)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302404 112107 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 4 1 6 5.1 Cc1nn(-c2c(F)cccc2CO)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
60154264 77019 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2086648 77019 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088060 77019 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
16131448 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
68182789 112113 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 488 5 0 6 5.2 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236477 112113 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 488 5 0 6 5.2 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302591 112113 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 488 5 0 6 5.2 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm500117r
70697390 77233 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 452 5 1 4 4.5 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088053 77233 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 452 5 1 4 4.5 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
70689063 77235 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088056 77235 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
44388473 158907 0 None - 1 Human 9.9 pKi = 9.9 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1952 69 33 31 -15.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410145 158907 0 None - 1 Human 9.9 pKi = 9.9 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1952 69 33 31 -15.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414767 211396 0 None 154 2 Human 9.9 pKi = 9.9 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44253565 141868 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
CHEMBL3889835 141868 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
16131448 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
1681 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
1688 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
44361543 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
56947112 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
CHEMBL396460 2796 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
70697391 77236 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088057 77236 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951808 77221 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088029 77221 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951808 77221 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088029 77221 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
58268595 112192 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 3 0 6 4.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236473 112192 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 3 0 6 4.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304363 112192 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 3 0 6 4.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
68182794 112106 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 5 0 6 5.7 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236482 112106 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 5 0 6 5.7 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302403 112106 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 5 0 6 5.7 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL410979 211098 0 None - 1 Human 9.8 pKi = 9.8 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
25208101 183331 0 None 41 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481367 183331 0 None 41 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
53319615 56994 0 None 1174 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650843 56994 0 None 1174 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
52951810 77225 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088033 77225 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
70695375 77917 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 466 5 0 4 4.9 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088052 77917 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 466 5 0 4 4.9 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2109867 77917 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 466 5 0 4 4.9 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
68182775 112125 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 3 0 5 5.8 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236480 112125 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 3 0 5 5.8 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302759 112125 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 3 0 5 5.8 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
52951810 77225 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088033 77225 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
58268569 112176 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 468 3 0 6 5.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236481 112176 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 468 3 0 6 5.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3304234 112176 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 468 3 0 6 5.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL269068 209022 0 None 56 5 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
25207950 183204 0 None 109 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480426 183204 0 None 109 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
16131448 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
58268591 112123 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 5 0 7 5.1 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236488 112123 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 5 0 7 5.1 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3302755 112123 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 5 0 7 5.1 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
11956520 120041 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326228 120041 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545629 120041 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
70682760 77240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 476 6 0 4 4.9 CN(C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
CHEMBL2088062 77240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 476 6 0 4 4.9 CN(C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
25208095 190605 0 None 18 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL518950 190605 0 None 18 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
46880032 7514 0 None 54 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1088036 7514 0 None 54 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
124565311 173488 0 None 165 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 minsDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 mins
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4544227 173488 0 None 165 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 minsDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 mins
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
16131448 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
1681 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
1688 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
44361543 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
56947112 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
CHEMBL396460 2796 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
25208245 183352 0 None 204 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481547 183352 0 None 204 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
52951674 77222 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088030 77222 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951674 77222 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088030 77222 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
10296561 1024 20 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
7361 1024 20 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL201945 1024 20 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL413944 211345 0 None - 1 Human 9.6 pKi = 9.6 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25208099 187776 0 None 41 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL501331 187776 0 None 41 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
9885004 168645 0 None 13 3 Rat 9.6 pKi = 9.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL440928 168645 0 None 13 3 Rat 9.6 pKi = 9.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
70691173 77916 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 0 6 2.4 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1cc(F)sc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088051 77916 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 0 6 2.4 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1cc(F)sc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2109866 77916 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 0 6 2.4 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1cc(F)sc12)Cn1cccn1 10.1021/jm201629q
15512229 3321 0 None 1 8 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
8864 3321 0 None 1 8 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
CHEMBL355202 3321 0 None 1 8 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
10047612 3460 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
1693 3460 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
CHEMBL559569 3460 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
10047612 3460 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
1693 3460 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
CHEMBL559569 3460 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
CHEMBL1162358 206764 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
16131448 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1681 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1688 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
44361543 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
56947112 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
CHEMBL396460 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
8868 3478 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 3478 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 3478 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
44438983 146639 0 None 16 4 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(F)c31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL392798 146639 0 None 16 4 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(F)c31)CC2 10.1016/j.bmcl.2007.01.069
134563655 173636 0 None 7 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 173636 0 None 7 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
25207948 183203 0 None 31 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480425 183203 0 None 31 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
10406239 120036 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326224 120036 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326226 120036 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3545624 120036 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
44414890 138640 0 None 1 3 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 445 4 3 6 2.5 C=CCN1CCC23c4c5ccc(O)c4O[C@@H]2/C(=N/NC(=O)c2ccccc2)CCC3(O)C1C5 10.1016/j.bmcl.2006.05.060
CHEMBL378753 138640 0 None 1 3 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 445 4 3 6 2.5 C=CCN1CCC23c4c5ccc(O)c4O[C@@H]2/C(=N/NC(=O)c2ccccc2)CCC3(O)C1C5 10.1016/j.bmcl.2006.05.060
CHEMBL409204 210994 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
15512237 203437 0 None 12 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2cccc(F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL78156 203437 0 None 12 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2cccc(F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
16131448 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
10047612 3460 14 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
1693 3460 14 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL559569 3460 14 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
11464846 77226 19 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 77226 19 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL1162357 206763 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
1682 2799 15 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
6324645 2799 15 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2799 15 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
58268645 112135 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 5 0 7 5.0 Cc1nn(-c2ncccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236483 112135 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 5 0 7 5.0 Cc1nn(-c2ncccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302938 112135 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 5 0 7 5.0 Cc1nn(-c2ncccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
10276738 171685 0 None 54 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4474536 171685 0 None 54 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
10763594 160718 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human nociceptin opioid receptorBinding affinity to human nociceptin opioid receptor
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL412098 160718 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human nociceptin opioid receptorBinding affinity to human nociceptin opioid receptor
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
10763594 160718 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/jm7009606
CHEMBL412098 160718 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/jm7009606
16131448 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
1681 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
1688 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
44361543 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
56947112 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
16131448 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 2796 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
60154200 77238 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088059 77238 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL261997 208769 6 None - 1 Mouse 9.4 pKi = 9.4 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44430038 86925 0 None 5 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 352 7 2 3 4.4 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233326 86925 0 None 5 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 352 7 2 3 4.4 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
23383556 178767 0 None 25 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473700 178767 0 None 25 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190623 189111 0 None 204 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL515575 189111 0 None 204 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
118662460 170552 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 354 4 0 2 4.4 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4458273 170552 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 354 4 0 2 4.4 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
10156591 120035 0 None 22 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 6 2 2 4.8 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccc(F)cc23)CC1 10.1021/ml500116x
CHEMBL3326223 120035 0 None 22 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 6 2 2 4.8 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccc(F)cc23)CC1 10.1021/ml500116x
CHEMBL3545623 120035 0 None 22 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 6 2 2 4.8 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccc(F)cc23)CC1 10.1021/ml500116x
1691 2067 14 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
5311194 2067 14 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
CHEMBL357076 2067 14 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
15512229 3321 0 None -1 8 Rat 9.4 pKi = 9.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(00)00111-6
8864 3321 0 None -1 8 Rat 9.4 pKi = 9.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(00)00111-6
CHEMBL355202 3321 0 None -1 8 Rat 9.4 pKi = 9.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(00)00111-6
CHEMBL411621 211195 0 None 301 2 Human 9.4 pKi = 9.4 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
11004121 106547 0 None 60 4 Human 9.4 pKi = 9.4 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 409 2 0 3 5.4 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCCC2)CC1 10.1021/jm0209174
CHEMBL315551 106547 0 None 60 4 Human 9.4 pKi = 9.4 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 409 2 0 3 5.4 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCCC2)CC1 10.1021/jm0209174
60154191 77231 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088041 77231 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088042 77231 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
24894426 185175 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL486644 185175 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL415584 211434 0 None - 1 Human 9.3 pKi = 9.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
16131448 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1681 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1688 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44361543 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
56947112 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL396460 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44297539 193004 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 394 3 0 2 5.6 CC(C)C1CCC(N2CCC3(CC2)C(c2ccccc2)C[C@H]2CN(C)C[C@H]23)CC1 10.1016/j.bmcl.2003.09.068
CHEMBL53256 193004 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 394 3 0 2 5.6 CC(C)C1CCC(N2CCC3(CC2)C(c2ccccc2)C[C@H]2CN(C)C[C@H]23)CC1 10.1016/j.bmcl.2003.09.068
19347356 120004 0 None -2 4 Rat 9.3 pKi = 9.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354545 120004 0 None -2 4 Rat 9.3 pKi = 9.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
9824565 87309 0 None 501 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233750 87309 0 None 501 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
9866158 87488 0 None 74 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233955 87488 0 None 74 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.062
44430042 153854 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 406 5 2 3 4.9 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL398794 153854 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 406 5 2 3 4.9 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44430044 154199 0 None 380 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL400035 154199 0 None 380 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
23383564 168773 0 None 3 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 366 8 2 3 4.8 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL441914 168773 0 None 3 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 366 8 2 3 4.8 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
25190602 178635 0 None 50 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL472669 178635 0 None 50 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
25190619 178716 0 None 123 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473279 178716 0 None 123 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190622 178896 0 None 131 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474096 178896 0 None 131 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190605 179900 0 None 15 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475310 179900 0 None 15 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190603 189214 0 None 57 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL516389 189214 0 None 57 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44437610 144974 0 None 42 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 144974 0 None 42 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
118722882 120030 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 7 1 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325879 120030 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 7 1 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545617 120030 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 7 1 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCCc2ccccc2)CC1 10.1021/ml500116x
118711485 120033 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 342 6 1 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)CCC2CCCC2)CC1 10.1021/ml500116x
CHEMBL3326220 120033 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 342 6 1 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)CCC2CCCC2)CC1 10.1021/ml500116x
CHEMBL3545621 120033 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 342 6 1 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)CCC2CCCC2)CC1 10.1021/ml500116x
11329662 95742 0 None 107 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL260767 95742 0 None 107 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
10022859 98700 1 None 10 4 Human 9.3 pKi = 9.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
CHEMBL281274 98700 1 None 10 4 Human 9.3 pKi = 9.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
15512228 67399 0 None 8 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranesDisplacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranes
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL1907858 67399 0 None 8 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranesDisplacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranes
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
10927662 106629 0 None 251 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 407 2 0 3 4.9 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H]3CCCC[C@@H]3C2)CC1 10.1021/jm0209174
CHEMBL316086 106629 0 None 251 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 407 2 0 3 4.9 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H]3CCCC[C@@H]3C2)CC1 10.1021/jm0209174
25208249 183373 0 None 194 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481707 183373 0 None 194 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL3809510 210518 0 None 616 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL None None None CC[C@H](C)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
68632142 153070 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 480 5 0 2 6.7 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3980782 153070 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 480 5 0 2 6.7 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL507269 212505 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
10430819 78212 0 None 363 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112345 78212 0 None 363 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
118711490 120043 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 373 2 1 2 4.9 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CC1)c1[nH]c3ccccc3c1CCN2C 10.1021/ml500117c
CHEMBL3326229 120043 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 373 2 1 2 4.9 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CC1)c1[nH]c3ccccc3c1CCN2C 10.1021/ml500117c
CHEMBL3545631 120043 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 373 2 1 2 4.9 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CC1)c1[nH]c3ccccc3c1CCN2C 10.1021/ml500117c
16131448 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1681 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1688 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44361543 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
56947112 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL396460 2796 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44426832 85264 0 None 14 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 5 1 2 5.3 CCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228848 85264 0 None 14 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 5 1 2 5.3 CCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430087 86431 0 None 309 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 615 8 1 5 5.9 CC(C)S(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232286 86431 0 None 309 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 615 8 1 5 5.9 CC(C)S(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
25190629 178526 0 None 41 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL471880 178526 0 None 41 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190604 188989 0 None 21 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514662 188989 0 None 21 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
46879580 5776 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079400 5776 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL427791 211624 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
1682 2799 15 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
6324645 2799 15 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2799 15 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
25207946 190694 0 None 91 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL519100 190694 0 None 91 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
10022859 98700 1 None 10 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL281274 98700 1 None 10 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
11014751 112132 0 None 87 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 2 0 3 5.0 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCC2)CC1 10.1021/jm0209174
CHEMBL330291 112132 0 None 87 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 2 0 3 5.0 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCC2)CC1 10.1021/jm0209174
44253418 151526 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3967435 151526 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
11761926 78209 0 None 380 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 437 6 0 3 5.9 CCCCN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1021/jm0209174
CHEMBL2112342 78209 0 None 380 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 437 6 0 3 5.9 CCCCN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1021/jm0209174
9997843 99191 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL284414 99191 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
9863568 141545 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430050 86574 0 None 234 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 454 6 2 3 5.8 CNCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232477 86574 0 None 234 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 454 6 2 3 5.8 CNCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44430040 86926 0 None 39 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 2 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233327 86926 0 None 39 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 2 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
25190625 178528 0 None 37 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL471882 178528 0 None 37 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190601 180248 0 None 56 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475707 180248 0 None 56 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190600 189053 0 None 75 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL515142 189053 0 None 75 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
118662189 174018 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 4 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4557245 174018 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 4 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
45102745 5951 0 None 97 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080485 5951 0 None 97 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44252989 145891 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
CHEMBL3921976 145891 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
25001412 62307 0 None 33 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783826 62307 0 None 33 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
53324890 56993 0 None 416 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650842 56993 0 None 416 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
10928037 78215 0 None 169 4 Human 9.1 pKi = 9.1 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 425 5 1 4 4.1 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCO)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112348 78215 0 None 169 4 Human 9.1 pKi = 9.1 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 425 5 1 4 4.1 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCO)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
1682 2799 15 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
6324645 2799 15 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
CHEMBL384755 2799 15 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
CHEMBL389521 210670 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm990075h
CHEMBL405648 210815 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
25190618 178715 0 None 218 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL473278 178715 0 None 218 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190599 189420 0 None 85 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL517167 189420 0 None 85 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44438988 90765 0 None 17 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(F)cccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240005 90765 0 None 17 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(F)cccc31)CC2 10.1016/j.bmcl.2007.01.069
118662074 170292 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 346 4 0 3 5.0 CN(C)C1(c2cccs2)CCC2(CCN(CC3CCCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4454146 170292 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 346 4 0 3 5.0 CN(C)C1(c2cccs2)CCC2(CCN(CC3CCCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
44253136 146776 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
CHEMBL3929120 146776 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
CHEMBL269029 209020 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44451649 95698 0 None 57 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260556 95698 0 None 57 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL412537 211245 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1cccc(F)c1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44430085 86420 0 None 162 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 601 8 1 5 5.5 CCS(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232285 86420 0 None 162 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 601 8 1 5 5.5 CCS(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
25190616 179710 0 None 223 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475094 179710 0 None 223 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190614 188965 0 None 37 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL514463 188965 0 None 37 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190613 189045 0 None 54 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL515091 189045 0 None 54 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
18782352 90687 0 None 38 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(F)cc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239824 90687 0 None 38 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(F)cc31)CC2 10.1016/j.bmcl.2007.01.069
11848225 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
11848225 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3545616 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
1682 2799 15 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
6324645 2799 15 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 2799 15 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
10000890 120106 0 None -3 4 Rat 9.0 pKi = 9.0 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 397 2 1 3 5.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354652 120106 0 None -3 4 Rat 9.0 pKi = 9.0 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 397 2 1 3 5.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
53322245 56999 0 None 288 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650848 56999 0 None 288 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
70690760 76297 0 None 85 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064160 76297 0 None 85 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL406905 210872 0 None - 1 Mouse 9.0 pKi = 9 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
44248674 102912 0 None 602 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084677 102912 0 None 602 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
10109899 85269 0 None 28 4 Human 9.0 pKi = 9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228857 85269 0 None 28 4 Human 9.0 pKi = 9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
25190615 178711 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473272 178711 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190606 178768 0 None 56 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473701 178768 0 None 56 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44437619 90783 0 None 22 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240074 90783 0 None 22 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437610 144974 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437610 144974 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL391487 144974 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 144974 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
10301207 148111 0 None 26 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393960 148111 0 None 26 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
11956680 120034 0 None -2 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325961 120034 0 None -2 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3545622 120034 0 None -2 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL265544 208898 0 None - 1 Mouse 9.0 pKi = 9 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL436732 211929 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
44430043 87106 0 None 66 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 450 5 2 3 5.0 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233536 87106 0 None 66 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 450 5 2 3 5.0 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
24894428 185735 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL487485 185735 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
44438961 144439 0 None 11 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 377 6 1 3 4.3 CCCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL391082 144439 0 None 11 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 377 6 1 3 4.3 CCCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
118662342 171079 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
CHEMBL4466096 171079 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
9925137 120038 0 None 8 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326222 120038 0 None 8 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3545626 120038 0 None 8 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
24798599 120047 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 346 2 2 2 4.6 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326232 120047 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 346 2 2 2 4.6 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545637 120047 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 346 2 2 2 4.6 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
58358709 125267 0 None 56 4 Human 9.0 pKi = 9.0 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 449 3 1 5 4.9 C[C@H]1C[C@H]2C[C@@H](C1)C[C@H](N1[C@H]3CCC[C@@H]1C[C@H](n1c(=O)c(C(=O)O)nc4ccccc41)C3)C2 nan
CHEMBL3647962 125267 0 None 56 4 Human 9.0 pKi = 9.0 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 449 3 1 5 4.9 C[C@H]1C[C@H]2C[C@@H](C1)C[C@H](N1[C@H]3CCC[C@@H]1C[C@H](n1c(=O)c(C(=O)O)nc4ccccc41)C3)C2 nan
1684 3298 17 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 3298 17 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 3298 17 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9997843 99191 0 None 8 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL284414 99191 0 None 8 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44451621 95454 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 0 8 5.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cscn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259263 95454 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 0 8 5.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cscn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
10430819 78212 0 None 363 4 Human 8.9 pKi = 8.9 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112345 78212 0 None 363 4 Human 8.9 pKi = 8.9 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
15512234 104955 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2cccc(Cl)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL312021 104955 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2cccc(Cl)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
68917692 113479 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 358 2 1 1 5.8 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CCCc3c4ccccc4[nH]c32)CC1 10.1021/ml500117c
CHEMBL3326231 113479 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 358 2 1 1 5.8 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CCCc3c4ccccc4[nH]c32)CC1 10.1021/ml500117c
44224242 147440 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
CHEMBL3934183 147440 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
25190624 90686 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL239822 90686 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190624 90686 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.01.069
CHEMBL239822 90686 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.01.069
46880033 7528 0 None 26 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC4(CCCCC4)C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1088171 7528 0 None 26 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC4(CCCCC4)C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
9905428 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
9905428 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
10714523 98637 1 None 22 4 Human 8.9 pKi = 8.9 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
CHEMBL280827 98637 1 None 22 4 Human 8.9 pKi = 8.9 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
25190621 178789 0 None 48 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL473898 178789 0 None 48 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190612 188970 0 None 47 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514489 188970 0 None 47 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
9947044 97806 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL27460 97806 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44439000 147926 0 None 34 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2007.01.069
CHEMBL393807 147926 0 None 34 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2007.01.069
9905428 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL101454 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
9905428 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL101454 4328 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
44451918 95634 0 None 31 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccs4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260169 95634 0 None 31 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccs4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
68633222 149590 0 None 27 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 6 0 2 6.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(F)c2)CC1 nan
CHEMBL3951319 149590 0 None 27 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 6 0 2 6.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(F)c2)CC1 nan
49843555 56995 0 None 138 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650844 56995 0 None 138 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
134578457 173373 0 None 309 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4541337 173373 0 None 309 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
25190617 178891 0 None 29 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL474092 178891 0 None 29 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
44438962 166033 0 None 16 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 391 6 1 3 4.6 CC(C)CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL428033 166033 0 None 16 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 391 6 1 3 4.6 CC(C)CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
19347398 119943 0 None -1 4 Rat 8.8 pKi = 8.8 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354065 119943 0 None -1 4 Rat 8.8 pKi = 8.8 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
44451595 95511 0 None 25 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccsc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259511 95511 0 None 25 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccsc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44252684 142864 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3898034 142864 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
15512243 102436 0 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL306150 102436 0 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
15512240 203353 0 None 19 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2ccc(Cl)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL77324 203353 0 None 19 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2ccc(Cl)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44252536 152747 0 None -6 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
CHEMBL3977883 152747 0 None -6 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
44430023 87081 0 None 79 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 372 5 2 3 4.2 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233503 87081 0 None 79 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 372 5 2 3 4.2 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
25190611 179387 0 None 23 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474687 179387 0 None 23 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
118662159 173134 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 5 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CC1)CC(=O)N(CCC1(C#N)CCC1)C2 10.1021/acsmedchemlett.6b00277
CHEMBL4536065 173134 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 5 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CC1)CC(=O)N(CCC1(C#N)CCC1)C2 10.1021/acsmedchemlett.6b00277
11315651 77228 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 403 5 0 5 3.1 CN(C)C(=O)C(Cc1cscn1)CN1CCC2(CC1)OCc1ccc(F)cc12 10.1021/jm201629q
CHEMBL2088037 77228 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 403 5 0 5 3.1 CN(C)C(=O)C(Cc1cscn1)CN1CCC2(CC1)OCc1ccc(F)cc12 10.1021/jm201629q
10961428 78213 0 None 102 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 453 5 0 3 5.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CC4CC4)C[C@@H]2CN3c2ccc(F)cc2)CC1 10.1021/jm0209174
CHEMBL2112346 78213 0 None 102 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 453 5 0 3 5.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CC4CC4)C[C@@H]2CN3c2ccc(F)cc2)CC1 10.1021/jm0209174
10950562 78214 0 None 81 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 457 4 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(c4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112347 78214 0 None 81 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 457 4 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(c4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
44451569 95938 0 None 58 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 535 10 0 9 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncsn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL261839 95938 0 None 58 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 535 10 0 9 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncsn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11848793 188725 0 None 22 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512414 188725 0 None 22 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
25190609 179036 0 None 34 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL474283 179036 0 None 34 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25208247 183353 0 None 89 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481548 183353 0 None 89 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
45102745 7462 0 None 117 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087657 7462 0 None 117 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44451649 95698 0 None 57 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260556 95698 0 None 57 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11626062 138407 0 None 79 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785095 138407 0 None 79 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL507653 212663 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
10766007 30666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 451 5 2 4 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C(F)(F)F)cc3)ccc2n1 10.1021/jm0002073
CHEMBL139776 30666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 451 5 2 4 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C(F)(F)F)cc3)ccc2n1 10.1021/jm0002073
10789513 31575 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 445 7 2 4 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL140640 31575 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 445 7 2 4 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
10765154 167721 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 6 2 4 5.9 CCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL434060 167721 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 6 2 4 5.9 CCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
9958643 87489 0 None 151 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 528 5 2 3 5.7 NCc1ccccc1C1(O)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233956 87489 0 None 151 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 528 5 2 3 5.7 NCc1ccccc1C1(O)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
25190628 188572 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL511161 188572 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL406097 210838 0 None - 1 Mouse 8.7 pKi = 8.7 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Br)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
60154191 77231 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088041 77231 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088042 77231 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
44451748 160473 0 None 20 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 9 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cncn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL411643 160473 0 None 20 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 9 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cncn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430083 86327 0 None 75 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 509 6 2 4 5.5 OC1(c2ccccc2CN2CCNCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232075 86327 0 None 75 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 509 6 2 4 5.5 OC1(c2ccccc2CN2CCNCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44574588 177851 0 None 54 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466067 177851 0 None 54 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
12986253 120028 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325881 120028 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545610 120028 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
19347402 119936 0 None 4 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 341 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL353990 119936 0 None 4 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 341 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL265801 208908 0 None - 1 Mouse 8.7 pKi = 8.7 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010221v
15512228 67399 0 None 8 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL1907858 67399 0 None 8 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44451650 95743 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL260768 95743 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL410396 211061 16 None -1 2 Mouse 8.0 pKi = 8 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
44252685 150749 0 None 1 2 Human 8.0 pKi = 8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 502 7 0 2 7.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)C(c2ccccc2)c2ccccc2)CC1 nan
CHEMBL3960588 150749 0 None 1 2 Human 8.0 pKi = 8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 502 7 0 2 7.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)C(c2ccccc2)c2ccccc2)CC1 nan
44248920 102905 0 None 27 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
CHEMBL3084667 102905 0 None 27 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
44413442 79518 0 None 26 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
CHEMBL212575 79518 0 None 26 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
118718290 114816 0 None 56 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 CNC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349274 114816 0 None 56 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 CNC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
11462727 188781 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL512896 188781 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
44574892 178076 0 None 33 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 506 6 1 2 7.2 CC(C)NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467699 178076 0 None 33 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 506 6 1 2 7.2 CC(C)NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
22725091 188812 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513171 188812 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76335142 102842 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084540 102842 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76335143 102848 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 437 4 1 3 6.0 N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084547 102848 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 437 4 1 3 6.0 N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76313424 102851 0 None 60 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 497 5 1 3 6.3 CC(=O)N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084550 102851 0 None 60 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 497 5 1 3 6.3 CC(=O)N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76335144 102852 0 None 74 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084551 102852 0 None 74 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76313425 102855 0 None 28 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 512 6 1 2 7.1 NC(=O)[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084554 102855 0 None 28 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 512 6 1 2 7.1 NC(=O)[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
15512239 203402 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 451 2 1 3 4.9 O=C1NCN(c2cccc(C(F)(F)F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL77877 203402 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 451 2 1 3 4.9 O=C1NCN(c2cccc(C(F)(F)F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44315305 203439 0 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 411 2 1 3 4.5 Cc1cc(C)cc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
CHEMBL78163 203439 0 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 411 2 1 3 4.5 Cc1cc(C)cc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
44437630 145017 0 None 6 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391518 145017 0 None 6 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
9922658 120046 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 308 5 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325751 120046 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 308 5 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545636 120046 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 308 5 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCc2ccccc2)CC1 10.1021/ml500116x
10713623 96515 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL26638 96515 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
11552010 138475 0 None 38 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
CHEMBL3785728 138475 0 None 38 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
52951941 83167 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204346 83167 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
129188459 174586 0 None 54 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4570328 174586 0 None 54 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
134563466 170716 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4460695 170716 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44391062 122096 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 122096 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
18782376 91329 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(Cl)cc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241085 91329 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(Cl)cc31)CC2 10.1016/j.bmcl.2007.01.069
44438964 146845 0 None 75 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 415 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL392969 146845 0 None 75 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 415 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
10654047 210873 16 None -2 2 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL406946 210873 16 None -2 2 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL407461 210906 0 None - 1 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
24799509 97319 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 360 3 1 2 4.3 CC(C)(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL271779 97319 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 360 3 1 2 4.3 CC(C)(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
44574707 178201 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 446 4 0 2 7.2 N#CC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468953 178201 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 446 4 0 2 7.2 N#CC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
15512242 102395 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
CHEMBL305861 102395 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
134134392 143151 0 None -331 3 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 309 3 1 2 4.2 Cc1ccc(C2(N(C)C)CCC(O)(c3ccccc3)CC2)cc1 nan
CHEMBL3900292 143151 0 None -331 3 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 309 3 1 2 4.2 Cc1ccc(C2(N(C)C)CCC(O)(c3ccccc3)CC2)cc1 nan
44426819 141457 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 292 3 1 3 3.2 N#CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL387493 141457 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 292 3 1 3 3.2 N#CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
70692893 76287 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 400 7 0 4 2.2 CCC(CC)N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064137 76287 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 400 7 0 4 2.2 CCC(CC)N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
44437610 144974 0 None 42 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 144974 0 None 42 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44252534 151771 0 None -3 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3969636 151771 0 None -3 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44337550 109184 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL322717 109184 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44252391 152379 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.5 CN(C)CC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3974883 152379 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.5 CN(C)CC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL143939 207020 17 None -3388 2 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmcl.2006.05.060
24799325 97240 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 432 5 1 2 5.9 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
CHEMBL271342 97240 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 432 5 1 2 5.9 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
118718273 114799 0 None 38 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 497 6 0 3 6.7 CN(C)C[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349257 114799 0 None 38 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 497 6 0 3 6.7 CN(C)C[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44224242 147440 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
CHEMBL3934183 147440 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
10286996 162787 0 None 38 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 364 5 1 2 4.8 N[C@@H](c1cc(F)cc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL419179 162787 0 None 38 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 364 5 1 2 4.8 N[C@@H](c1cc(F)cc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
90656666 110449 0 None -186 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 481 5 2 5 4.8 CC[C@](O)([C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
CHEMBL3262088 110449 0 None -186 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 481 5 2 5 4.8 CC[C@](O)([C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
46880240 5961 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3nccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080521 5961 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3nccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
9836463 96372 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 313 3 1 2 3.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL26521 96372 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 313 3 1 2 3.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
68631642 148074 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 415 4 1 2 6.2 Cc1c(C2(N3CCCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
CHEMBL3939293 148074 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 415 4 1 2 6.2 Cc1c(C2(N3CCCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
46879478 5398 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076208 5398 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337230 6782 0 None 3 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 300 4 1 2 4.2 CC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108417 6782 0 None 3 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 300 4 1 2 4.2 CC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
54581495 62305 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 434 7 0 5 4.1 O=C(OCCCN1CCC2(CC1)OCc1ccccc12)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783822 62305 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 434 7 0 5 4.1 O=C(OCCCN1CCC2(CC1)OCc1ccccc12)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
44253136 146776 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
CHEMBL3929120 146776 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
134144744 150075 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 436 6 1 3 6.2 CCCC(=O)OC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
CHEMBL3955335 150075 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 436 6 1 3 6.2 CCCC(=O)OC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
44391156 64524 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 7 2 6 4.8 Cc1ccc(Cl)c(OC(C(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182144 64524 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 7 2 6 4.8 Cc1ccc(Cl)c(OC(C(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44593575 177895 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466438 177895 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
105104 3828 36 None -776 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
1655 3828 36 None -776 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
1656 3828 36 None -776 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
CHEMBL440765 3828 36 None -776 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
68632581 147807 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
CHEMBL3937167 147807 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
10134077 101235 0 None 40 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.9 CCN1C(=O)N(C2CCN(CC3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL29953 101235 0 None 40 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.9 CCN1C(=O)N(C2CCN(CC3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
10159203 65264 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183355 65264 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44391062 122096 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 122096 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44426836 141572 0 None 15 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388314 141572 0 None 15 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
20481138 86411 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232273 86411 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718288 114814 0 None 11 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 481 6 1 4 6.0 COc1cccc([C@@]2(CN)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
CHEMBL3349272 114814 0 None 11 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 481 6 1 4 6.0 COc1cccc([C@@]2(CN)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
118718301 114828 0 None 123 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349286 114828 0 None 123 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894531 178541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 Cc1ccccc1C1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL471982 178541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 Cc1ccccc1C1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
11326750 185717 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
CHEMBL487458 185717 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
44574963 177929 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 7 2 3 6.1 CC(O)CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466694 177929 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 7 2 3 6.1 CC(O)CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574789 177963 0 None 91 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
CHEMBL466919 177963 0 None 91 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
70419 74645 42 None 17 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 321 3 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL203356 74645 42 None 17 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 321 3 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
155569552 175630 0 None 61 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 509 10 5 5 3.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)[C@@H](N)CCCNC(=N)N)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4594096 175630 0 None 61 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 509 10 5 5 3.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)[C@@H](N)CCCNC(=N)N)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
46879537 6092 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081191 6092 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
24798598 112078 7 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3301613 112078 7 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325959 112078 7 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
155544763 172774 0 None 7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL4527189 172774 0 None 7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
90655975 110506 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262548 110506 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
21345766 79689 0 None 1 3 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 449 3 1 7 2.3 CN1CC[C@]23c4c5ccc(OC(=O)C(C)(C)C)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414864 79689 0 None 1 3 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 449 3 1 7 2.3 CN1CC[C@]23c4c5ccc(OC(=O)C(C)(C)C)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL213228 79689 0 None 1 3 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 449 3 1 7 2.3 CN1CC[C@]23c4c5ccc(OC(=O)C(C)(C)C)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
73350483 90018 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387193 90018 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
44438966 91325 0 None 50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 411 4 1 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL241079 91325 0 None 50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 411 4 1 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
25134075 127642 0 None 218 2 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2ccc(F)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665421 127642 0 None 218 2 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2ccc(F)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
70684433 76292 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 420 5 0 4 2.6 Cc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064145 76292 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 420 5 0 4 2.6 Cc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
11371415 4278 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 4.1 O=C1Cc2ccccc2N1C1CCN(C2CCCc3ccccc32)CC1 10.1021/jm034249d
CHEMBL101118 4278 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 4.1 O=C1Cc2ccccc2N1C1CCN(C2CCCc3ccccc32)CC1 10.1021/jm034249d
44451648 95697 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncnn4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260555 95697 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncnn4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
9889948 31445 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 413 6 2 5 5.0 COc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
CHEMBL140519 31445 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 413 6 2 5 5.0 COc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
44430045 87307 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccc(C(c2ccc(C)cc2)N2CCC(O)(c3ccccc3CN)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL233748 87307 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccc(C(c2ccc(C)cc2)N2CCC(O)(c3ccccc3CN)CC2)cc1 10.1016/j.bmcl.2007.03.062
10338496 120029 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 286 3 0 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCCCC2)CC1 10.1021/ml500116x
CHEMBL3325883 120029 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 286 3 0 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCCCC2)CC1 10.1021/ml500116x
CHEMBL3545612 120029 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 286 3 0 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCCCC2)CC1 10.1021/ml500116x
44339530 108029 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL320058 108029 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
10292091 96305 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 361 3 0 2 4.6 CCN1C(=O)N(C2CCN(C3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL26464 96305 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 361 3 0 2 4.6 CCN1C(=O)N(C2CCN(C3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
46879629 5781 0 None 28 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079417 5781 0 None 28 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44391012 167737 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 467 6 1 5 6.5 Cc1ccc(Cl)c(OC2(CCN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL434150 167737 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 467 6 1 5 6.5 Cc1ccc(Cl)c(OC2(CCN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
46880153 5422 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 358 6 1 5 2.2 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076499 5422 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 358 6 1 5 2.2 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44391119 131504 0 None -5 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 435 8 1 5 6.0 CC(C)c1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL369540 131504 0 None -5 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 435 8 1 5 6.0 CC(C)c1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44337231 9058 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 390 5 1 2 5.8 Cc1ccc(C(c2ccc(C)cc2)N2CC[C@H]2[C@H](N)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL110138 9058 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 390 5 1 2 5.8 Cc1ccc(C(c2ccc(C)cc2)N2CC[C@H]2[C@H](N)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(02)00652-2
44413409 77875 0 None -5 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 324 3 1 1 5.2 Clc1ccc2[nH]cc(C3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL210770 77875 0 None -5 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 324 3 1 1 5.2 Clc1ccc2[nH]cc(C3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44430026 87785 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 351 8 1 2 5.6 CCCCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL234773 87785 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 351 8 1 2 5.6 CCCCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
54584440 62303 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 447 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783820 62303 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 447 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
44252987 143979 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
CHEMBL3907138 143979 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
11743914 109164 0 None -114 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL322515 109164 0 None -114 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
118718264 114789 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 7 0 2 8.0 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@](Cc1ccccc1)(CN1CCCC1)C2 10.1016/j.bmcl.2008.10.088
CHEMBL3349247 114789 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 7 0 2 8.0 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@](Cc1ccccc1)(CN1CCCC1)C2 10.1016/j.bmcl.2008.10.088
44402713 134644 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL371984 134644 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
44253564 144898 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3914240 144898 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
44252247 148895 0 None -8 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 4 1 2 3.2 CC(=O)NCC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3945941 148895 0 None -8 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 4 1 2 3.2 CC(=O)NCC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
44451573 168848 0 None -2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 575 10 0 9 6.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C(C)(C)C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL442469 168848 0 None -2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 575 10 0 9 6.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C(C)(C)C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
118718297 114824 0 None 20 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 522 7 1 3 6.8 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
CHEMBL3349282 114824 0 None 20 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 522 7 1 3 6.8 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
24735827 91272 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccn1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240895 91272 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccn1)CC2 10.1016/j.bmcl.2007.01.069
44339525 8527 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109509 8527 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
44339525 8527 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL109509 8527 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2004.08.032
44390989 165327 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL424971 165327 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
24776402 97119 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
CHEMBL270756 97119 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
44426829 85257 0 None 10 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228794 85257 0 None 10 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.061
44430080 86326 0 None 25 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 511 7 3 3 5.9 CCNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232074 86326 0 None 25 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 511 7 3 3 5.9 CCNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
118718302 114829 0 None 38 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 7 1 2 7.1 CC(=O)NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349287 114829 0 None 38 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 7 1 2 7.1 CC(=O)NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
11256620 178546 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL471994 178546 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
76335145 102853 0 None 79 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 529 5 1 4 7.0 COC(=O)N[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084552 102853 0 None 79 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 529 5 1 4 7.0 COC(=O)N[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44574958 188583 0 None 74 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 513 5 1 4 6.5 COC(=O)NC1(c2ccc(F)cn2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL511232 188583 0 None 74 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 513 5 1 4 6.5 COC(=O)NC1(c2ccc(F)cn2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
22558157 110505 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262547 110505 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
44437646 89899 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238602 89899 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437648 147088 0 None 8 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393138 147088 0 None 8 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437628 170088 0 None 10 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL445154 170088 0 None 10 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44402486 123803 0 None -2 3 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL363619 123803 0 None -2 3 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
15411840 119952 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL354163 119952 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
25190592 187620 0 None 56 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
CHEMBL499169 187620 0 None 56 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
25190630 178556 0 None 12 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL472086 178556 0 None 12 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
71624387 90020 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387195 90020 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
9803475 77227 22 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 77227 22 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
12986256 113427 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 218 2 1 2 2.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](N)CC1 10.1021/ml500116x
CHEMBL3325882 113427 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 218 2 1 2 2.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](N)CC1 10.1021/ml500116x
10715726 32131 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 6 2 3 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCCc3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL141078 32131 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 6 2 3 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCCc3ccccc3)ccc2n1 10.1021/jm0002073
76335141 102840 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 533 5 1 3 6.5 NC(=O)[C@@]1(c2ccc(C(F)(F)F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084537 102840 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 533 5 1 3 6.5 NC(=O)[C@@]1(c2ccc(C(F)(F)F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
10156336 98877 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 5 0 2 4.9 CCCC1CCC(N2CCC(N3C(=O)N(CC)[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL282376 98877 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 5 0 2 4.9 CCCC1CCC(N2CCC(N3C(=O)N(CC)[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
9923726 99163 0 None 11 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 333 2 1 2 3.9 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL284217 99163 0 None 11 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 333 2 1 2 3.9 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
44391104 64668 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182328 64668 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44426837 85268 0 None 19 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228856 85268 0 None 19 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2007.03.061
44402487 69450 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL193614 69450 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL411621 211195 0 None -301 2 Mouse 6.9 pKi = 6.9 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm990075h
44252684 142864 0 None 5 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3898034 142864 0 None 5 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
10133332 100711 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 363 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL29571 100711 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 363 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2003.11.083
44391138 65117 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
CHEMBL182995 65117 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
44339505 9309 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 344 3 0 2 5.1 N#CC1(c2ccccc2)CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111628 9309 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 344 3 0 2 5.1 N#CC1(c2ccccc2)CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(03)00665-6
122179051 120779 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3580675 120779 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44431782 87382 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 350 4 1 4 4.2 OC1(c2nccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233820 87382 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 350 4 1 4 4.2 OC1(c2nccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
70690756 76284 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 450 7 0 5 2.6 CCOc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064132 76284 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 450 7 0 5 2.6 CCOc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
44430012 87615 0 None 2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 371 5 1 2 5.3 CCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL234543 87615 0 None 2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 371 5 1 2 5.3 CCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
134563695 171587 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 3 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(C(N)=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4473383 171587 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 3 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(C(N)=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10269001 85246 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228690 85246 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
10269001 85246 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL228690 85246 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
10269001 85246 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2009.03.031
CHEMBL228690 85246 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2009.03.031
44574587 177850 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
CHEMBL466066 177850 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
76313427 102862 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)nc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084561 102862 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)nc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
24970041 127662 0 None 13 4 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
CHEMBL3665440 127662 0 None 13 4 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
10669670 34416 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3Cl)ccc2n1 10.1021/jm0002073
CHEMBL142999 34416 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3Cl)ccc2n1 10.1021/jm0002073
70684436 76294 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064157 76294 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
44253564 144898 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3914240 144898 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
1627 2546 18 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
1845 2546 18 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
5288826 2546 18 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
CHEMBL70 2546 18 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
DB00295 2546 18 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
24776411 97235 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 342 4 1 2 4.0 CNC(=O)C1(c2ccccc2)CCN(C2CCC(C(C)C)CC2)CC1 10.1021/jm7009606
CHEMBL271322 97235 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 342 4 1 2 4.0 CNC(=O)C1(c2ccccc2)CCN(C2CCC(C(C)C)CC2)CC1 10.1021/jm7009606
118705898 112355 0 None -8511 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 484 4 2 5 3.6 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1Cc1ccccc1 10.1016/j.bmc.2014.05.065
CHEMBL3309515 112355 0 None -8511 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 484 4 2 5 3.6 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1Cc1ccccc1 10.1016/j.bmc.2014.05.065
44252242 149578 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3951213 149578 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44426834 85266 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228850 85266 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.061
9797246 91273 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cccnc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240896 91273 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cccnc1)CC2 10.1016/j.bmcl.2007.01.069
56681954 65359 0 None -43 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 5 2 5 5.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccc(C(C)(C)C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834412 65359 0 None -43 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 5 2 5 5.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccc(C(C)(C)C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44426817 85245 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 6 1 3 3.7 CCOCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228687 85245 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 6 1 3 3.7 CCOCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44337252 5167 0 None 3 4 Human 5.9 pKi = 5.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 322 9 1 2 5.2 CCCCC(CCCC)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106359 5167 0 None 3 4 Human 5.9 pKi = 5.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 322 9 1 2 5.2 CCCCC(CCCC)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
11165726 111112 0 None -6 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 408 3 0 2 5.4 CC(c1ccc2c(c1)Cc1ccccc1-2)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
CHEMBL328411 111112 0 None -6 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 408 3 0 2 5.4 CC(c1ccc2c(c1)Cc1ccccc1-2)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
44426806 167685 0 None 10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 295 4 1 2 4.1 CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL433814 167685 0 None 10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 295 4 1 2 4.1 CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
24776406 95547 0 None 8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL259681 95547 0 None 8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
10336926 86286 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 333 4 1 3 4.4 OC1(c2ccco2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231874 86286 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 333 4 1 3 4.4 OC1(c2ccco2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
134578518 172427 0 None 7 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 397 7 2 4 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNCCO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4518220 172427 0 None 7 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 397 7 2 4 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNCCO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44252681 141939 0 None -758 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CN(C)C1(c2cccc(F)c2)CCC(C)(CNC(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3890424 141939 0 None -758 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CN(C)C1(c2cccc(F)c2)CCC(C)(CNC(=O)/C=C/c2ccccc2)CC1 nan
44337131 106830 0 None 36 4 Human 7.9 pKi = 7.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@H](c1cccc(C(F)(F)F)c1)[C@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL317479 106830 0 None 36 4 Human 7.9 pKi = 7.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@H](c1cccc(C(F)(F)F)c1)[C@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44391094 64129 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181389 64129 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44248791 102893 0 None 46 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084648 102893 0 None 46 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
44426810 85526 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 7 1 2 5.3 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230253 85526 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 7 1 2 5.3 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
10089987 86324 0 None 53 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccc(F)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232066 86324 0 None 53 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccc(F)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44574630 188823 0 None 109 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 534 6 1 3 7.4 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCN2Cc2ccccc2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL513303 188823 0 None 109 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 534 6 1 3 7.4 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCN2Cc2ccccc2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44438916 90775 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 4 2.7 O=C1NCN(c2ccccc2)C12CCN(Cc1ccsc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240033 90775 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 4 2.7 O=C1NCN(c2ccccc2)C12CCN(Cc1ccsc1)CC2 10.1016/j.bmcl.2007.01.069
18782384 168800 0 None 14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 375 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL442090 168800 0 None 14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 375 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44438967 91326 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241080 91326 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2007.01.069
44575092 178096 0 None 5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL467933 178096 0 None 5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
44402413 123804 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 460 2 0 5 6.3 N#Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL363622 123804 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 460 2 0 5 6.3 N#Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
44430021 87079 0 None 5 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 368 4 1 3 4.6 N#Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL233501 87079 0 None 5 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 368 4 1 3 4.6 N#Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
122179064 120882 0 None -13182 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581762 120882 0 None -13182 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
24776400 156398 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cc(F)ccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
CHEMBL407275 156398 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cc(F)ccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
44253419 146718 0 None 5 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3928651 146718 0 None 5 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44395286 66655 0 None -489 2 Human 6.8 pKi = 6.8 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 531 7 1 4 6.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL186938 66655 0 None -489 2 Human 6.8 pKi = 6.8 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 531 7 1 4 6.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL427617 211598 0 None - 1 Human 7.8 pKi = 7.8 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
69016300 153292 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
CHEMBL3982651 153292 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
10601891 96329 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 513 5 0 4 5.2 O=C(CN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O)c1ccccc1 10.1021/jm991129q
CHEMBL26483 96329 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 513 5 0 4 5.2 O=C(CN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O)c1ccccc1 10.1021/jm991129q
11757207 86575 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 9 2 4 5.9 CCCS(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232478 86575 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 9 2 4 5.9 CCCS(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44430033 147366 0 None 50 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 363 4 1 3 5.1 Cc1ccsc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL393356 147366 0 None 50 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 363 4 1 3 5.1 Cc1ccsc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718277 114803 0 None 51 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349261 114803 0 None 51 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
76316935 102833 0 None 9 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084530 102833 0 None 9 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76327872 102843 0 None 30 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)cc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084541 102843 0 None 30 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)cc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46880031 7353 0 None 39 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.3 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1086749 7353 0 None 39 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.3 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44437644 91351 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241155 91351 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
16739256 148131 0 None 61 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 457 2 1 3 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2007.01.069
CHEMBL393980 148131 0 None 61 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 457 2 1 3 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2007.01.069
71624266 90014 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387189 90014 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
10697286 99329 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 519 4 0 3 6.2 O=C1N(Cc2ccccc2)CN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL285377 99329 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 519 4 0 3 6.2 O=C1N(Cc2ccccc2)CN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
11233481 4250 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 3 0 2 4.1 CC1(C)C2CCC(CN3CCC(N4C(=O)Cc5ccccc54)CC3)C1C2 10.1021/jm034249d
CHEMBL100938 4250 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 3 0 2 4.1 CC1(C)C2CCC(CN3CCC(N4C(=O)Cc5ccccc54)CC3)C1C2 10.1021/jm034249d
155537352 171719 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 348 4 0 3 4.4 CCCC(=O)N1CCC2(CCC(c3sccc3C)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4474989 171719 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 348 4 0 3 4.4 CCCC(=O)N1CCC2(CCC(c3sccc3C)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
11164004 108051 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL320182 108051 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL414792 211399 0 None - 1 Mouse 7.8 pKi = 7.8 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](N)CNCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/jm990075h
15512236 104396 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
CHEMBL311185 104396 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
25190627 189188 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL516187 189188 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
134578342 172482 0 None 16 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
CHEMBL4519453 172482 0 None 16 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
118705899 112356 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 498 5 2 5 3.7 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CCc1ccccc1 10.1016/j.bmc.2014.05.065
CHEMBL3309516 112356 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 498 5 2 5 3.7 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CCc1ccccc1 10.1016/j.bmc.2014.05.065
118662129 174965 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 342 6 0 2 4.1 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
CHEMBL4578716 174965 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 342 6 0 2 4.1 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
44337357 7648 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1ccc(Cl)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL108904 7648 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1ccc(Cl)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
57502889 127655 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 2 0 3 4.0 CN1C(=O)CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
CHEMBL3665434 127655 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 2 0 3 4.0 CN1C(=O)CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
44339393 110190 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 351 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL326030 110190 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 351 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
44437601 90183 0 None 7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 90183 0 None 7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437643 154086 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 10 1 7 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL399393 154086 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 10 1 7 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
57502894 127651 0 None 3 2 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 439 5 1 3 5.5 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O nan
CHEMBL3665430 127651 0 None 3 2 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 439 5 1 3 5.5 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O nan
44574393 178070 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL467676 178070 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
54585396 62306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 420 8 0 4 4.6 c1ccc(CN2CCC[C@@H]2COCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
CHEMBL1783823 62306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 420 8 0 4 4.6 c1ccc(CN2CCC[C@@H]2COCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
56681955 65363 0 None -18 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4cc(Br)c(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834416 65363 0 None -18 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4cc(Br)c(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44437629 90179 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 10 1 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238796 90179 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 10 1 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10291377 98629 0 None 67 4 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL280778 98629 0 None 67 4 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
44426814 152912 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 1 2 5.0 OC1(c2ccccc2)CCN(C(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL397945 152912 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 1 2 5.0 OC1(c2ccccc2)CCN(C(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430022 87080 0 None 11 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233502 87080 0 None 11 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
42629117 177964 0 None 7 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466921 177964 0 None 7 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76313423 102844 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2nc(F)ccc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084542 102844 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2nc(F)ccc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
56658044 65360 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834413 65360 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
46879477 5807 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 454 6 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccccc3-c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1079562 5807 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 454 6 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccccc3-c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44413408 77518 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 368 2 1 1 5.8 Fc1ccc2c(C3=CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL209399 77518 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 368 2 1 1 5.8 Fc1ccc2c(C3=CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
118711156 120040 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 4 1 2 4.0 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325746 120040 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 4 1 2 4.0 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545628 120040 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 4 1 2 4.0 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(Cc2ccccc2)CC1 10.1021/ml500116x
44252683 144584 0 None -2 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
CHEMBL3911970 144584 0 None -2 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
10388166 85298 0 None 22 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 433 7 0 2 7.0 c1ccc(COC2(c3ccccc3)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
CHEMBL229018 85298 0 None 22 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 433 7 0 2 7.0 c1ccc(COC2(c3ccccc3)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
44252987 143979 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
CHEMBL3907138 143979 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
44413396 138400 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 448 5 2 5 4.4 N#Cc1ccc2c(c1)c(C1=CCN(C3Cc4cccc5cccc3c45)CC1)cn2C[C@H](O)CN 10.1016/j.bmcl.2006.03.094
CHEMBL378453 138400 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 448 5 2 5 4.4 N#Cc1ccc2c(c1)c(C1=CCN(C3Cc4cccc5cccc3c45)CC1)cn2C[C@H](O)CN 10.1016/j.bmcl.2006.03.094
59159346 128505 0 None - 1 Human 4.8 pKi = 4.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)NC(=O)CC(=O)N2C1CCN(C2/C=C\CCCCC2)CC1 nan
CHEMBL3670295 128505 0 None - 1 Human 4.8 pKi = 4.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)NC(=O)CC(=O)N2C1CCN(C2/C=C\CCCCC2)CC1 nan
44430029 86241 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 7 1 2 5.6 OC1(CCCc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231664 86241 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 7 1 2 5.6 OC1(CCCc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
18666969 32646 3 None - 1 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 0.7 CN1CC[C@]23c4c5ccc(OS(=O)(=O)O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414680 32646 3 None - 1 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 0.7 CN1CC[C@]23c4c5ccc(OS(=O)(=O)O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL1415 32646 3 None - 1 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 0.7 CN1CC[C@]23c4c5ccc(OS(=O)(=O)O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44252386 151468 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 462 9 1 3 5.8 CCCCC1(CNS(=O)(=O)c2ccc(Cl)cc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3966922 151468 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 462 9 1 3 5.8 CCCCC1(CNS(=O)(=O)c2ccc(Cl)cc2)CCC(c2ccccc2)(N(C)C)CC1 nan
10043439 149048 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 2 5.2 OC1(C2CCCCC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL394695 149048 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 2 5.2 OC1(C2CCCCC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718269 114795 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 457 5 2 3 5.8 NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349253 114795 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 457 5 2 3 5.8 NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718291 114817 0 None 87 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349275 114817 0 None 87 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894425 178540 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
CHEMBL471981 178540 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
76316937 102857 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 7 2 3 6.5 NC(=O)C[C@@]1(Cc2ccc(O)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084556 102857 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 7 2 3 6.5 NC(=O)C[C@@]1(Cc2ccc(O)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44575043 188787 0 None 28 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 471 5 2 3 5.3 NC(=O)C1(C2CCCCN2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL512962 188787 0 None 28 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 471 5 2 3 5.3 NC(=O)C1(C2CCCCN2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44438921 90852 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 3.6 CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL240216 90852 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 3.6 CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
52951939 83172 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204354 83172 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
44451593 156090 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 10 0 8 6.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4csc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL406926 156090 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 10 0 8 6.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4csc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL410167 211046 0 None - 1 Mouse 7.8 pKi = 7.8 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(I)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44252101 150668 0 None 36 3 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 308 4 1 2 4.1 CNC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3959941 150668 0 None 36 3 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 308 4 1 2 4.1 CNC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
118662042 173807 0 None -38 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 6 0 2 4.6 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4552146 173807 0 None -38 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 6 0 2 4.6 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL2371034 208248 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(N)=O)CC[C@@H]1C(C)(C)C 10.1021/jm020078l
118718282 114808 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 507 6 1 3 6.5 CC(=O)NC[C@]1(c2ncccc2C)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349266 114808 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 507 6 1 3 6.5 CC(=O)NC[C@]1(c2ncccc2C)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25129302 128504 0 None 69 2 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 409 2 1 3 4.9 O=C1CC(=O)N([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c2ccccc2N1 nan
CHEMBL3670294 128504 0 None 69 2 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 409 2 1 3 4.9 O=C1CC(=O)N([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c2ccccc2N1 nan
44430013 147748 0 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 6 1 2 5.7 CCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL393675 147748 0 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 6 1 2 5.7 CCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
44252835 153643 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3985824 153643 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
57502946 127658 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 464 3 1 5 3.7 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCCCC1 nan
CHEMBL3665437 127658 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 464 3 1 5 3.7 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCCCC1 nan
57502948 128508 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 486 5 2 5 4.0 O=C(NCc1ccccc1)C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1 nan
CHEMBL3670298 128508 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 486 5 2 5 4.0 O=C(NCc1ccccc1)C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1 nan
CHEMBL262928 208798 0 None - 1 Mouse 5.8 pKi = 5.8 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
58358756 125266 0 None 11 4 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.8 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C23CCCC(CCC2)C3)c1=O nan
CHEMBL3647961 125266 0 None 11 4 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.8 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C23CCCC(CCC2)C3)c1=O nan
44253700 152092 0 None 23 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 380 8 1 3 4.6 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCCCO)CC1 nan
CHEMBL3972320 152092 0 None 23 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 380 8 1 3 4.6 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCCCO)CC1 nan
44248918 102886 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccnc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)c1 10.1021/jm9008218
CHEMBL3084635 102886 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccnc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)c1 10.1021/jm9008218
16665918 79324 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211722 79324 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44426812 86161 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 351 8 1 2 5.7 CCCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL231607 86161 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 351 8 1 2 5.7 CCCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
11256620 178546 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL471994 178546 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
46880239 5960 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 458 6 1 6 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(OC)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080520 5960 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 458 6 1 6 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(OC)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10160920 66624 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL186773 66624 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
127034554 138480 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 375 2 1 2 3.5 NC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3785839 138480 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 375 2 1 2 3.5 NC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
25190583 178785 0 None 25 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL473884 178785 0 None 25 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
54756989 65357 0 None -14 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 5 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834410 65357 0 None -14 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 5 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
9927928 90024 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387199 90024 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
11581029 138524 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 346 2 0 2 4.0 CN1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3786338 138524 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 346 2 0 2 4.0 CN1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
87655565 150687 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 5 1 4 5.4 CN(C)C1(c2ccccc2)CCC(C(=N)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
CHEMBL3960085 150687 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 5 1 4 5.4 CN(C)C1(c2ccccc2)CCC(C(=N)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
24799146 97270 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL271542 97270 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
44430018 87073 0 None 16 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
CHEMBL233494 87073 0 None 16 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
10178311 78686 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 387 3 0 2 4.9 CCN1C(=O)N(C2CCN(C3CCC4CCCCC4C3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL2113273 78686 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 387 3 0 2 4.9 CCN1C(=O)N(C2CCN(C3CCC4CCCCC4C3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
44337437 5122 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106155 5122 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
118662342 171079 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
CHEMBL4466096 171079 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
24776396 96994 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cccc(F)c23)CC1 10.1021/jm7009606
CHEMBL270133 96994 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cccc(F)c23)CC1 10.1021/jm7009606
24800188 155937 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 346 4 1 2 3.9 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL406758 155937 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 346 4 1 2 3.9 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
46880155 7576 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 5 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1088569 7576 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 5 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
90656667 110460 0 None -245 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 479 5 2 5 4.6 CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
CHEMBL3262362 110460 0 None -245 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 479 5 2 5 4.6 CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
44394419 65864 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184451 65864 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
44394320 123111 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 6 1 4 4.1 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL361926 123111 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 6 1 4 4.1 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
90655978 110509 0 None -18 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262551 110509 0 None -18 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
44426818 85250 0 None 3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 4 1 4 2.9 COC(=O)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228736 85250 0 None 3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 4 1 4 2.9 COC(=O)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44297727 193295 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL54603 193295 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
44252387 147175 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 6 0 2 4.8 CN(C)CC1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3932117 147175 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 6 0 2 4.8 CN(C)CC1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44426807 85517 0 None 12 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 309 5 1 2 4.5 CCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230145 85517 0 None 12 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 309 5 1 2 4.5 CCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44593576 188606 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511373 188606 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76327875 102847 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 515 6 1 3 6.1 NC(=O)[C@@]1(c2cc(CF)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084545 102847 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 515 6 1 3 6.1 NC(=O)[C@@]1(c2cc(CF)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437640 90787 0 None 14 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240086 90787 0 None 14 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
25190582 189174 0 None 34 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL516077 189174 0 None 34 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10407144 192808 0 None -7 4 Human 7.7 pKi = 7.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
CHEMBL52604 192808 0 None -7 4 Human 7.7 pKi = 7.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
10432317 141053 0 None 1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 4 1 7 1.6 CCC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414843 141053 0 None 1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 4 1 7 1.6 CCC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL385048 141053 0 None 1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 4 1 7 1.6 CCC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL414767 211396 0 None -154 2 Mouse 7.7 pKi = 7.7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm990075h
44253569 148658 0 None 8 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 419 4 1 2 5.9 Cc1c(C2(N3CCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
CHEMBL3943962 148658 0 None 8 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 419 4 1 2 5.9 Cc1c(C2(N3CCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
44252534 151771 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3969636 151771 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44336905 167353 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 346 5 1 2 4.7 N[C@@H](c1cccc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL431445 167353 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 346 5 1 2 4.7 N[C@@H](c1cccc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44391075 122541 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360972 122541 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
57502947 127659 0 None - 1 Human 5.7 pKi = 5.7 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 466 3 1 6 2.6 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCOCC1 nan
CHEMBL3665438 127659 0 None - 1 Human 5.7 pKi = 5.7 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 466 3 1 6 2.6 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCOCC1 nan
90656664 110459 0 None -204 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 499 6 2 5 4.7 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL3262361 110459 0 None -204 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 499 6 2 5 4.7 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
44337362 171885 0 None 4 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 358 6 1 3 4.6 COc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL448155 171885 0 None 4 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 358 6 1 3 4.6 COc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
44593575 177895 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466438 177895 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
97333 85516 74 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 267 3 1 2 3.2 OC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230141 85516 74 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 267 3 1 2 3.2 OC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL413178 211295 0 None - 1 Mouse 6.7 pKi = 6.7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None Cc1ccc(C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm990075h
45271534 193576 0 None 162 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551111 193576 0 None 162 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45269032 194500 0 None 208 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
CHEMBL561373 194500 0 None 208 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
44413330 79507 0 None 85 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 383 2 1 4 4.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2O)c2cccnc21 10.1016/j.bmcl.2006.03.094
CHEMBL212525 79507 0 None 85 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 383 2 1 4 4.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2O)c2cccnc21 10.1016/j.bmcl.2006.03.094
9844540 85278 0 None 128 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228911 85278 0 None 128 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
9863568 141545 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430079 86284 0 None 99 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 497 6 3 3 5.5 CNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231866 86284 0 None 99 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 497 6 3 3 5.5 CNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44574745 178017 0 None 13 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 493 5 2 2 6.5 CNC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467314 178017 0 None 13 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 493 5 2 2 6.5 CNC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
18782378 91330 0 None 46 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(Cl)cccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241086 91330 0 None 46 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(Cl)cccc31)CC2 10.1016/j.bmcl.2007.01.069
9848110 170069 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysis
ChEMBL 373 4 2 5 4.4 Cc1ccc2nc(/C=C/c3ccccn3)nc(N[C@H]3CC[C@@H](N)C[C@H]3C)c2c1 10.1016/j.ejmech.2018.12.012
CHEMBL4451306 170069 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysis
ChEMBL 373 4 2 5 4.4 Cc1ccc2nc(/C=C/c3ccccn3)nc(N[C@H]3CC[C@@H](N)C[C@H]3C)c2c1 10.1016/j.ejmech.2018.12.012
44437602 90209 0 None 14 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 90209 0 None 14 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437638 90785 0 None 22 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240084 90785 0 None 22 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437656 145170 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
CHEMBL391631 145170 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
44437654 145190 0 None 16 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391650 145190 0 None 16 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10225083 165832 0 None 8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 165832 0 None 8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
118711486 113478 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326225 113478 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
155533462 171257 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4468676 171257 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
12985907 57240 0 None 3 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL166445 57240 0 None 3 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
60154189 77229 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088038 77229 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088039 77229 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
11123873 78208 0 None 70 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 494 6 0 5 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCN4CCOCC4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112341 78208 0 None 70 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 494 6 0 5 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCN4CCOCC4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
9947044 97806 0 None 15 4 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL27460 97806 0 None 15 4 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
25190610 179211 0 None 16 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474485 179211 0 None 16 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190586 179713 0 None 239 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475096 179713 0 None 239 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
24800107 191255 0 None 7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
CHEMBL519925 191255 0 None 7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
90655971 110500 0 None 19 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262542 110500 0 None 19 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
11826819 78210 1 None 72 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 471 5 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(Cc4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112343 78210 1 None 72 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 471 5 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(Cc4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
25190593 189136 0 None 77 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL515829 189136 0 None 77 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
129188454 169255 0 None 25 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439811 169255 0 None 25 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10937810 78211 0 None 117 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 381 3 1 3 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CNC[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112344 78211 0 None 117 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 381 3 1 3 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CNC[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
9846747 118485 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL342580 118485 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL405212 210793 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
10363496 162613 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 398 2 2 3 4.3 Oc1ccc2c3c1O[C@H]1Cc4c([nH]c5ccccc45)[C@H]4[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm00038a019
CHEMBL418105 162613 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 398 2 2 3 4.3 Oc1ccc2c3c1O[C@H]1Cc4c([nH]c5ccccc45)[C@H]4[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm00038a019
44430084 86328 0 None 63 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 523 6 1 4 5.8 CN1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232076 86328 0 None 63 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 523 6 1 4 5.8 CN1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
11516508 138457 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785560 138457 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
9937777 174775 0 None 114 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL457451 174775 0 None 114 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
129188462 175822 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4465668 175822 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4596017 175822 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
9825723 116165 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 428 6 2 6 4.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc([N+](=O)[O-])cc3)ccc2n1 10.1021/jm0002073
CHEMBL337128 116165 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 428 6 2 6 4.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc([N+](=O)[O-])cc3)ccc2n1 10.1021/jm0002073
1691 2067 14 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
5311194 2067 14 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
CHEMBL357076 2067 14 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
10155966 188678 0 None 40 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL511920 188678 0 None 40 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
25190598 90844 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL240215 90844 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
10323169 178792 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL473904 178792 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
25190598 90844 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240215 90844 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
118662456 172392 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 365 5 0 3 4.8 CN(C)C1(c2ccccc2)CCC2(CCN(CCC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4517646 172392 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 365 5 0 3 4.8 CN(C)C1(c2ccccc2)CCC2(CCN(CCC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
46879579 5946 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080464 5946 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44451619 95404 0 None 32 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 0 9 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncon4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259048 95404 0 None 32 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 0 9 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncon4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44438922 91345 0 None 9 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 363 5 1 3 4.0 CCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL241112 91345 0 None 9 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 363 5 1 3 4.0 CCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
11544795 138474 0 None 120 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785718 138474 0 None 120 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
46178991 125262 0 None 1071 4 Human 8.6 pKi = 8.6 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.6 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
CHEMBL3647958 125262 0 None 1071 4 Human 8.6 pKi = 8.6 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.6 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
44253417 152143 0 None 199 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 402 6 0 4 4.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccn(C)n2)CC1 nan
CHEMBL3972755 152143 0 None 199 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 402 6 0 4 4.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccn(C)n2)CC1 nan
10618605 98169 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL27716 98169 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
10593778 98772 0 None 10 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
CHEMBL28172 98772 0 None 10 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
44570675 183238 0 None 4 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 325 2 0 3 5.2 CC1(N2CCC(n3cnc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480619 183238 0 None 4 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 325 2 0 3 5.2 CC1(N2CCC(n3cnc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
46879581 5808 0 None 42 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079571 5808 0 None 42 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL412479 211238 0 None - 1 Mouse 8.6 pKi = 8.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/jm990075h
44451543 95971 0 None 41 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cocn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL262064 95971 0 None 41 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cocn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
25190587 190165 0 None 181 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL518325 190165 0 None 181 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10718869 33763 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 461 5 2 4 5.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Br)cc3)ccc2n1 10.1021/jm0002073
CHEMBL142454 33763 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 461 5 2 4 5.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Br)cc3)ccc2n1 10.1021/jm0002073
44438993 147887 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(Cl)c31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL393781 147887 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(Cl)c31)CC2 10.1016/j.bmcl.2007.01.069
10385808 65796 0 None 33 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 33 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44252249 148487 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 420 6 1 3 4.7 CN(C)C1(c2ccccc2)CCC(C)(CNS(=O)(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL3942616 148487 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 420 6 1 3 4.7 CN(C)C1(c2ccccc2)CCC(C)(CNS(=O)(=O)c2ccc(Cl)cc2)CC1 nan
44574585 178042 0 None 21 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL467488 178042 0 None 21 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
46880238 5957 0 None 51 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 442 5 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(C)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080508 5957 0 None 51 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 442 5 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(C)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
25190594 174679 0 None 87 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL457244 174679 0 None 87 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10574643 99116 0 None 2 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283910 99116 0 None 2 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
11795019 98149 0 None 3 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)cccc3C1)CC2 10.1021/jm991129q
CHEMBL27699 98149 0 None 3 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)cccc3C1)CC2 10.1021/jm991129q
118662291 171819 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 320 5 0 3 4.6 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4476510 171819 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 320 5 0 3 4.6 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
46879538 6093 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081192 6093 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
90655973 110503 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262545 110503 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL414541 211379 0 None - 1 Human 7.7 pKi = 7.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
44253419 146718 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3928651 146718 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44391133 64779 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL182410 64779 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
118718280 114806 0 None 21 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 509 8 1 4 6.7 CCNC[C@]1(c2cccc(OC)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349264 114806 0 None 21 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 509 8 1 4 6.7 CCNC[C@]1(c2cccc(OC)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25235412 114818 0 None 38 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349276 114818 0 None 38 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718292 114819 0 None 45 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 508 6 1 3 7.0 COC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349277 114819 0 None 45 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 508 6 1 3 7.0 COC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894647 185977 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 351 3 1 4 3.2 Cc1ccccc1N1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL487826 185977 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 351 3 1 4 3.2 Cc1ccccc1N1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
44574791 177992 0 None 30 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467119 177992 0 None 30 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
25235412 102830 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084527 102830 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437642 91307 0 None 12 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240941 91307 0 None 12 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437645 91352 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL241157 91352 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
118711486 113478 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326225 113478 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
10669669 35025 0 None - 1 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3cccc(Cl)c3)ccc2n1 10.1021/jm0002073
CHEMBL143605 35025 0 None - 1 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3cccc(Cl)c3)ccc2n1 10.1021/jm0002073
22562137 90023 0 None -2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387198 90023 0 None -2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
10836379 162604 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL418020 162604 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
134563704 176050 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4451073 176050 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4597933 176050 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
3655995 108245 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
CHEMBL320874 108245 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
3655995 108245 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL320874 108245 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.5b00982
3655995 108245 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL320874 108245 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
46179069 125263 0 None 117 3 Human 6.7 pKi = 6.7 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
CHEMBL3647959 125263 0 None 117 3 Human 6.7 pKi = 6.7 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
25190579 189031 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514965 189031 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
66911347 113378 0 None -4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 295 3 1 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(c2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325745 113378 0 None -4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 295 3 1 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(c2ccccc2)CC1 10.1021/ml500116x
44253421 150812 0 None -7 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 4 1 2 5.4 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
CHEMBL3961206 150812 0 None -7 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 4 1 2 5.4 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
44252839 146434 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 338 5 1 3 4.1 CNC1(c2ccccc2)CCC(c2ccc(OC)cc2)(N(C)C)CC1 nan
CHEMBL3926333 146434 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 338 5 1 3 4.1 CNC1(c2ccccc2)CCC(c2ccc(OC)cc2)(N(C)C)CC1 nan
44253565 141868 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
CHEMBL3889835 141868 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
24776398 97433 0 None 8 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 368 1 0 2 4.6 CN1Cc2ccccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
CHEMBL272390 97433 0 None 8 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 368 1 0 2 4.6 CN1Cc2ccccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
44426842 142712 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 499 4 1 2 6.3 OC1(c2ccccc2)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389666 142712 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 499 4 1 2 6.3 OC1(c2ccccc2)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
24894533 185716 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 2 4 3.0 Cc1cc(F)ccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
CHEMBL487457 185716 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 2 4 3.0 Cc1cc(F)ccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
46879536 6265 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 5 1 3 3.9 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1082092 6265 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 5 1 3 3.9 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44451518 159354 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 8 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cc(C)on4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL410706 159354 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 8 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cc(C)on4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44253416 148564 0 None 11 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 631 11 0 9 7.8 COc1ccc(Oc2nc(Oc3ccc(OC)cc3)nc(N(C)C3(c4ccccc4)CCC(c4ccccc4)(N(C)C)CC3)n2)cc1 nan
CHEMBL3943194 148564 0 None 11 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 631 11 0 9 7.8 COc1ccc(Oc2nc(Oc3ccc(OC)cc3)nc(N(C)C3(c4ccccc4)CCC(c4ccccc4)(N(C)C)CC3)n2)cc1 nan
118718293 114820 0 None 12 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 6 0 2 7.1 CC(=O)N(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349278 114820 0 None 12 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 6 0 2 7.1 CC(=O)N(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
9848990 188566 1 None -812 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 467 4 2 5 4.4 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 10.1021/jm401964y
CHEMBL2368861 188566 1 None -812 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 467 4 2 5 4.4 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 10.1021/jm401964y
CHEMBL511142 188566 1 None -812 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 467 4 2 5 4.4 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 10.1021/jm401964y
9848990 188566 1 None -812 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 467 4 2 5 4.4 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 10.1021/acs.jmedchem.5b00130
CHEMBL2368861 188566 1 None -812 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 467 4 2 5 4.4 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 10.1021/acs.jmedchem.5b00130
CHEMBL511142 188566 1 None -812 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 467 4 2 5 4.4 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 10.1021/acs.jmedchem.5b00130
71624267 90015 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 312 3 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(CC2CCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387190 90015 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 312 3 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(CC2CCCCC2)CC1 10.1016/j.bmcl.2013.03.101
44366689 120450 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -0.7 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1S[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL356210 120450 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -0.7 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1S[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
44426822 136463 0 None 27 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccn2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL374602 136463 0 None 27 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccn2)CC1 10.1016/j.bmcl.2007.03.061
131534 164092 19 None -19498 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 544 7 1 3 6.1 CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL421665 164092 19 None -19498 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 544 7 1 3 6.1 CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
46879627 6195 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 385 3 1 4 3.4 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1081741 6195 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 385 3 1 4 3.4 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
134563500 175480 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 436 5 1 4 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(N)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4590786 175480 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 436 5 1 4 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(N)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
118662169 173289 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 314 3 0 2 3.3 CC(=O)N1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4539568 173289 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 314 3 0 2 3.3 CC(=O)N1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
44430028 86240 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 5 1 2 4.8 OC1(Cc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231661 86240 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 5 1 2 4.8 OC1(Cc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44391069 63555 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL180499 63555 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
10500922 97151 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cc(Cl)ccc3C1)CC2 10.1021/jm991129q
CHEMBL27093 97151 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cc(Cl)ccc3C1)CC2 10.1021/jm991129q
60154191 77231 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088041 77231 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088042 77231 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
71454460 78251 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@H]2CC3CCC2C3)CC1 10.1021/jm034249d
CHEMBL2112407 78251 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@H]2CC3CCC2C3)CC1 10.1021/jm034249d
44248790 102898 0 None 40 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccc(Br)cn1)C2 10.1021/jm9008218
CHEMBL3084656 102898 0 None 40 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccc(Br)cn1)C2 10.1021/jm9008218
44574850 188752 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 6 1 3 6.1 COc1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
CHEMBL512612 188752 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 6 1 3 6.1 COc1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
76316936 102836 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 6 1 4 5.5 COc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084533 102836 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 6 1 4 5.5 COc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
54756990 65358 0 None -10 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834411 65358 0 None -10 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
46879668 5876 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 456 5 1 3 4.3 CNC(=O)CN1Cc2ccccc2N(C2CCN(Cc3ccc(C)c4ccccc34)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079941 5876 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 456 5 1 3 4.3 CNC(=O)CN1Cc2ccccc2N(C2CCN(Cc3ccc(C)c4ccccc34)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44437613 146346 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL392548 146346 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
25134076 127643 0 None 36 4 Human 7.6 pKi = 7.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 3 1 4 3.5 CC(C)C1CCC(N2CCC(n3c(=O)c(=O)[nH]c4ccccc43)CC2)CC1 nan
CHEMBL3665422 127643 0 None 36 4 Human 7.6 pKi = 7.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 3 1 4 3.5 CC(C)C1CCC(N2CCC(n3c(=O)c(=O)[nH]c4ccccc43)CC2)CC1 nan
44339374 110095 0 None -56 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL325536 110095 0 None -56 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
44426831 85258 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228795 85258 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2007.03.061
10137134 91260 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240870 91260 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
10110916 65915 0 None 24 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184646 65915 0 None 24 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44402566 165717 0 None -23 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 478 3 0 5 6.5 CN(C)c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL427007 165717 0 None -23 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 478 3 0 5 6.5 CN(C)c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
46879628 5780 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 396 4 1 4 2.8 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079416 5780 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 396 4 1 4 2.8 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
46879993 6129 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 370 4 1 5 2.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1081375 6129 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 370 4 1 5 2.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
57502905 127647 0 None - 1 Human 6.6 pKi = 6.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccc(F)c2N1 nan
CHEMBL3665426 127647 0 None - 1 Human 6.6 pKi = 6.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccc(F)c2N1 nan
9947155 65960 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 363 2 1 3 3.7 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184864 65960 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 363 2 1 3 3.7 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
44248915 102904 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 468 5 0 3 7.6 CSc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084666 102904 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 468 5 0 3 7.6 CSc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
24776408 156849 0 None 173 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 358 2 1 2 4.0 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL407846 156849 0 None 173 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 358 2 1 2 4.0 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
9863568 141545 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430008 150453 0 None 30 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2cccc(F)c2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL395838 150453 0 None 30 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2cccc(F)c2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
22970051 152715 0 None 11 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 6 1 2 4.8 CCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL397761 152715 0 None 11 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 6 1 2 4.8 CCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
15541261 91131 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL240657 91131 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
15541261 91131 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240657 91131 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
44437652 90182 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238819 90182 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
155542684 172568 0 None 41 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4521436 172568 0 None 41 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
134563496 173971 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4556227 173971 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
68632578 147889 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 6 0 3 3.9 CN(C)C(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3937815 147889 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 6 0 3 3.9 CN(C)C(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44394283 65817 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184260 65817 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44339500 7371 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 387 3 1 2 5.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL108695 7371 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 387 3 1 2 5.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
25190578 179414 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474708 179414 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
69016300 153292 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
CHEMBL3982651 153292 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
10194236 106768 0 None 28 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL316961 106768 0 None 28 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
56668405 65361 0 None -35 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Br)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834414 65361 0 None -35 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Br)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44391103 65225 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
CHEMBL183135 65225 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
10070040 98820 4 None -169 3 Human 7.6 pKi = 7.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 408 7 0 4 3.9 CCC(=O)N(c1ccccc1)[C@@]1(C(=O)OC)CCN(CCc2ccccc2)C[C@H]1C 10.1021/jm991129q
CHEMBL28198 98820 4 None -169 3 Human 7.6 pKi = 7.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 408 7 0 4 3.9 CCC(=O)N(c1ccccc1)[C@@]1(C(=O)OC)CCN(CCc2ccccc2)C[C@H]1C 10.1021/jm991129q
44248792 102897 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 438 4 1 3 6.6 Oc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084655 102897 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 438 4 1 3 6.6 Oc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
10091033 146580 0 None 38 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 377 4 1 2 5.4 OC1(c2ccc(Cl)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL392753 146580 0 None 38 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 377 4 1 2 5.4 OC1(c2ccc(Cl)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718272 114798 0 None 53 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 511 6 1 3 6.3 CC(=O)NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349256 114798 0 None 53 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 511 6 1 3 6.3 CC(=O)NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894425 178540 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
CHEMBL471981 178540 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
134563698 171155 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 426 6 2 3 4.9 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4467156 171155 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 426 6 2 3 4.9 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
122179056 120874 0 None -2454 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581752 120874 0 None -2454 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
118718283 114809 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 548 7 1 4 7.0 NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349267 114809 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 548 7 1 4 7.0 NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44402627 71479 0 None -7 3 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 504 3 0 5 6.2 O=C1CCN1c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL196932 71479 0 None -7 3 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 504 3 0 5 6.2 O=C1CCN1c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
44438971 90682 0 None 6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(Cl)c1)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239819 90682 0 None 6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(Cl)c1)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2007.01.069
44391134 122784 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL361576 122784 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44248919 102901 0 None 213 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
CHEMBL3084661 102901 0 None 213 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
24894653 188742 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 392 3 0 4 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C3(C2)OCCO3)CC1 10.1021/jm701590h
CHEMBL512530 188742 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 392 3 0 4 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C3(C2)OCCO3)CC1 10.1021/jm701590h
11781971 96180 0 None 3 3 Rat 7.6 pKi = 7.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 313 2 1 3 2.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL263575 96180 0 None 3 3 Rat 7.6 pKi = 7.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 313 2 1 3 2.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL413516 211316 0 None - 1 Mouse 7.6 pKi = 7.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm990075h
44252539 153319 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 4 0 3 4.5 CN(C)C1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
CHEMBL3982887 153319 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 4 0 3 4.5 CN(C)C1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
44438975 90685 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(F)c1)c1cccc(F)c1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239821 90685 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(F)c1)c1cccc(F)c1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL411168 211109 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None Cc1ccc(CNCC(=O)NCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm990075h
CHEMBL425456 211576 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)CNCC(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/jm990075h
CHEMBL438234 212000 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
11327115 206371 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 402 4 0 2 5.8 CC(c1ccc(C2CCCCC2)cc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
CHEMBL97979 206371 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 402 4 0 2 5.8 CC(c1ccc(C2CCCCC2)cc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
46880115 7422 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 446 5 1 5 3.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(c4ccccc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087277 7422 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 446 5 1 5 3.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(c4ccccc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337232 108118 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 518 5 1 2 6.7 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Br)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL320582 108118 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 518 5 1 2 6.7 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Br)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(02)00652-2
46880151 7433 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 5 1 5 2.0 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087369 7433 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 5 1 5 2.0 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
46880152 7434 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 5 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087370 7434 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 5 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337461 108031 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 498 5 1 2 7.2 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(C(F)(F)F)c1)c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(02)00652-2
CHEMBL320061 108031 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 498 5 1 2 7.2 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(C(F)(F)F)c1)c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(02)00652-2
44337229 9093 0 None 60 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL110379 9093 0 None 60 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
24776403 160745 0 None 70 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL412290 160745 0 None 70 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
44426833 143733 0 None 7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL390498 143733 0 None 7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.061
25190584 189164 0 None 27 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL516024 189164 0 None 27 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179059 120877 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 517 6 2 6 4.7 COc1ccc([C@@H](O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(O)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 10.1021/acs.jmedchem.5b00130
CHEMBL3581755 120877 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 517 6 2 6 4.7 COc1ccc([C@@H](O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(O)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 10.1021/acs.jmedchem.5b00130
70690757 76288 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064139 76288 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
70690758 76289 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2F)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064140 76289 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2F)CC1 10.1016/j.ejmech.2012.07.021
71624269 90017 0 None -11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387192 90017 0 None -11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
1647 1281 39 None -43 10 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
5462471 1281 39 None -43 10 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
CHEMBL113995 1281 39 None -43 10 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
CHEMBL38874 1281 39 None -43 10 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
24800015 97207 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL271187 97207 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
44394345 126758 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 397 2 1 3 2.9 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL365870 126758 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 397 2 1 3 2.9 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
21345764 79297 0 None 2 3 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 435 4 1 7 1.9 CC(C)C(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414863 79297 0 None 2 3 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 435 4 1 7 1.9 CC(C)C(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL211576 79297 0 None 2 3 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 435 4 1 7 1.9 CC(C)C(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
10395965 106269 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144469 106269 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
44430009 168194 0 None 10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
CHEMBL437380 168194 0 None 10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
118718275 114801 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 499 6 2 3 6.0 CC(=O)NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349259 114801 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 499 6 2 3 6.0 CC(=O)NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718286 114812 0 None 28 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 571 6 1 3 6.9 CC(=O)NC[C@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349270 114812 0 None 28 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 571 6 1 3 6.9 CC(=O)NC[C@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
155536757 171649 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 362 4 0 3 4.7 Cc1ccsc1C1(N(C)C)CCC2(CCN(C(=O)CC(C)C)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4474067 171649 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 362 4 0 3 4.7 Cc1ccsc1C1(N(C)C)CCC2(CCN(C(=O)CC(C)C)C2)CC1 10.1021/acsmedchemlett.6b00277
127043001 139823 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808398 139823 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
71461579 78023 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@@H]2CC3CCC2C3)CC1 10.1021/jm034249d
CHEMBL2111608 78023 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@@H]2CC3CCC2C3)CC1 10.1021/jm034249d
44248788 102899 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 412 4 0 3 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cnco1)C2 10.1021/jm9008218
CHEMBL3084657 102899 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 412 4 0 3 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cnco1)C2 10.1021/jm9008218
1614 2449 37 None -186 7 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
443363 2449 37 None -186 7 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
CHEMBL13786 2449 37 None -186 7 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
DB12668 2449 37 None -186 7 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
44391081 62262 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL178318 62262 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
46879578 5945 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080463 5945 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44297435 193313 0 None -12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL54735 193313 0 None -12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
44394324 65809 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184234 65809 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44451572 158175 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccncc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL409351 158175 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccncc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11187225 178576 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL472168 178576 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
44391023 63535 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 399 6 1 5 4.8 Cc1ccc(Cl)c(OCCCN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL180402 63535 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 399 6 1 5 4.8 Cc1ccc(Cl)c(OCCCN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44574851 177901 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 548 6 1 3 7.0 NC(=O)C1(c2ccc(OC(F)(F)F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466469 177901 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 548 6 1 3 7.0 NC(=O)C1(c2ccc(OC(F)(F)F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
70692895 76291 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 411 5 0 3 3.7 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(C2CCCCC2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064143 76291 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 411 5 0 3 3.7 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(C2CCCCC2)CC1 10.1016/j.ejmech.2012.07.021
44248916 102909 0 None 58 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccnc1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084672 102909 0 None 58 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccnc1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
118718271 114797 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 469 5 1 3 6.1 NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349255 114797 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 469 5 1 3 6.1 NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
76324309 102834 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084531 102834 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46880237 5956 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080507 5956 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44437647 89898 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238600 89898 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437641 90971 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 13 1 7 5.2 CCCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240298 90971 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 13 1 7 5.2 CCCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
11393860 4369 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
CHEMBL101676 4369 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
118662117 170722 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 332 4 0 2 4.1 CN(C)C1(C2CCCC2)CCC2(CCN(C(=O)CC3CC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4460776 170722 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 332 4 0 2 4.1 CN(C)C1(C2CCCC2)CCC2(CCN(C(=O)CC3CC3)C2)CC1 10.1021/acsmedchemlett.6b00277
44451696 95434 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nc(C)no4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259157 95434 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nc(C)no4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11624970 138598 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 374 2 0 2 3.9 CC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3787051 138598 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 374 2 0 2 3.9 CC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
16665917 79349 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211846 79349 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
10171862 120039 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325749 120039 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545627 120039 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@H](OCc2ccccc2)CC1 10.1021/ml500116x
57502908 127653 0 None - 1 Human 6.5 pKi = 6.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 0 5 3.9 CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
CHEMBL3665432 127653 0 None - 1 Human 6.5 pKi = 6.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 0 5 3.9 CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
66911347 146273 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 295 3 1 2 3.9 CN(C)C1(c2ccccc2)CCC(O)(c2ccccc2)CC1 nan
CHEMBL3924824 146273 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 295 3 1 2 3.9 CN(C)C1(c2ccccc2)CCC(O)(c2ccccc2)CC1 nan
44252989 145891 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
CHEMBL3921976 145891 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
44426816 85244 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 311 5 1 3 3.4 COCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228686 85244 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 311 5 1 3 3.4 COCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
46879630 5782 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.3 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1079418 5782 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.3 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44252988 145593 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3919659 145593 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44593576 188606 0 None 6 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511373 188606 0 None 6 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44391124 95978 0 None 19 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL262104 95978 0 None 19 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
45268153 194450 0 None 102 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL561115 194450 0 None 102 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
44426843 85286 0 None 102 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228964 85286 0 None 102 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44426827 143445 0 None 48 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1cccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.061
CHEMBL390279 143445 0 None 48 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1cccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.061
44574631 177924 0 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466679 177924 0 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574538 188607 0 None 13 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 6.0 OC1(c2cccnc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511374 188607 0 None 13 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 6.0 OC1(c2cccnc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574708 188844 0 None 40 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 465 5 1 2 6.7 O=C(O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513471 188844 0 None 40 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 465 5 1 2 6.7 O=C(O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76324308 102829 0 None 28 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084526 102829 0 None 28 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76320666 102856 0 None 63 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 510 7 1 2 7.0 NC(=O)C[C@@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084555 102856 0 None 63 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 510 7 1 2 7.0 NC(=O)C[C@@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76309740 102860 0 None 23 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084559 102860 0 None 23 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437649 90181 0 None 39 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238818 90181 0 None 39 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437601 90183 0 None 7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 90183 0 None 7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437605 90443 0 None 37 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239260 90443 0 None 37 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437637 91451 0 None 22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241357 91451 0 None 22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437606 144973 0 None 45 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391486 144973 0 None 45 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
70696991 76293 0 None 22 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064156 76293 0 None 22 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
24776395 97538 0 None 154 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 2 0 2 4.2 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL272852 97538 0 None 154 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 2 0 2 4.2 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2ccccc23)CC1 10.1021/jm7009606
127033703 138492 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3785952 138492 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
86279209 110502 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262544 110502 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
25190596 177105 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL464191 177105 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44438917 154458 0 None 5 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 355 3 1 3 3.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL401451 154458 0 None 5 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 355 3 1 3 3.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
10837001 98185 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 443 2 0 3 4.6 CN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
CHEMBL27729 98185 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 443 2 0 3 4.6 CN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
15411840 168063 0 None 2 4 Rat 8.5 pKi = 8.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL436243 168063 0 None 2 4 Rat 8.5 pKi = 8.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
44451779 166137 0 None 67 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL428253 166137 0 None 67 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
9932834 177955 0 None 6 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 437 4 1 2 6.6 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466847 177955 0 None 6 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 437 4 1 2 6.6 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
90655972 110501 0 None 8 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262543 110501 0 None 8 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
11152739 188646 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
CHEMBL511658 188646 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
25190590 176211 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL460636 176211 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44438920 146754 0 None 14 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 335 3 1 3 3.2 CC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL392893 146754 0 None 14 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 335 3 1 3 3.2 CC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
46880116 7423 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 4 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087278 7423 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 4 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44451517 95425 0 None 15 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 546 10 0 8 5.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c(C)noc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259120 95425 0 None 15 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 546 10 0 8 5.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c(C)noc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
127034292 138536 0 None 95 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3786469 138536 0 None 95 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
44574629 188243 0 None 213 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL506634 188243 0 None 213 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
25190626 188573 0 None 38 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL511162 188573 0 None 38 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL428668 211707 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1F)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44561020 178596 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL472304 178596 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
25190591 189476 0 None 263 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL517265 189476 0 None 263 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
11956573 120045 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 1 2 5.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)SCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326230 120045 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 1 2 5.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)SCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545633 120045 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 1 2 5.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)SCCc1c3ccccc3[nH]c12 10.1021/ml500117c
10385808 65796 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44451837 158992 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 1 7 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c[nH]cn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL410257 158992 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 1 7 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c[nH]cn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
70688697 76296 0 None 36 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064159 76296 0 None 36 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
25190595 187760 0 None 70 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL501088 187760 0 None 70 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44451542 95970 0 None 21 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncco4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL262062 95970 0 None 21 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncco4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44394381 66631 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL186822 66631 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10042904 162759 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL418980 162759 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
10042904 90012 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387187 90012 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL429363 211768 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
15512235 103035 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
CHEMBL308522 103035 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
15512238 162800 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 461 2 1 3 4.6 O=C1NCN(c2cccc(Br)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL419272 162800 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 461 2 1 3 4.6 O=C1NCN(c2cccc(Br)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44337379 7634 0 None 60 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108893 7634 0 None 60 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
24894430 185979 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 O[C@H]1C[C@H](CN2CCC(c3ccccc3)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL487827 185979 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 O[C@H]1C[C@H](CN2CCC(c3ccccc3)CC2)CCc2cccnc21 10.1021/jm701590h
44402603 133045 0 None -2 3 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL371207 133045 0 None -2 3 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
44339540 8845 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 369 3 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109803 8845 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 369 3 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
10194236 106768 0 None 28 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL316961 106768 0 None 28 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
118718296 114823 0 None 67 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 510 6 1 2 6.9 CC(=O)NC[C@]1(c2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349281 114823 0 None 67 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 510 6 1 2 6.9 CC(=O)NC[C@]1(c2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44574848 177993 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 498 5 1 2 6.8 NC(=O)C1(c2ccc(Cl)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467131 177993 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 498 5 1 2 6.8 NC(=O)C1(c2ccc(Cl)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76313421 102837 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 480 5 2 4 5.1 NC(=O)[C@@]1(c2ccc(N)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084534 102837 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 480 5 2 4 5.1 NC(=O)[C@@]1(c2ccc(N)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
10158555 188506 0 None 4 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL510201 188506 0 None 4 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
45102745 5950 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080484 5950 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
70692894 76290 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 473 5 0 3 4.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2C(F)(F)F)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064141 76290 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 473 5 0 3 4.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2C(F)(F)F)CC1 10.1016/j.ejmech.2012.07.021
134563699 175492 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4591048 175492 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44402482 139959 0 None -16 3 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 534 4 0 6 6.2 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(CN5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL381000 139959 0 None -16 3 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 534 4 0 6 6.2 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(CN5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
10427620 148119 0 None 36 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 344 4 1 3 4.2 OC1(c2ccccn2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL393971 148119 0 None 36 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 344 4 1 3 4.2 OC1(c2ccccn2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44574706 188257 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 5 0 1 7.6 FCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL506803 188257 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 5 0 1 7.6 FCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL407671 210919 0 None - 1 Mouse 6.5 pKi = 6.5 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL412606 211252 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL428167 211664 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm990075h
44391052 129134 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL367367 129134 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
25129300 127648 0 None 117 2 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cc(F)ccc2N1 nan
CHEMBL3665427 127648 0 None 117 2 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cc(F)ccc2N1 nan
19347398 58399 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL168513 58399 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
44337459 5238 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL106785 5238 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(02)00652-2
9925737 85525 0 None 12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 281 3 1 2 3.7 CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230249 85525 0 None 12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 281 3 1 2 3.7 CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44426823 136465 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccnc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL374603 136465 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccnc2)CC1 10.1016/j.bmcl.2007.03.061
44253418 151526 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3967435 151526 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
10274330 66325 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL185415 66325 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
118718270 114796 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 532 7 0 2 7.6 O=C1CCCN1C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349254 114796 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 532 7 0 2 7.6 O=C1CCCN1C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
90663953 106271 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144471 106271 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
44337551 7784 0 None 57 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108995 7784 0 None 57 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44366822 120986 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL358403 120986 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
44248789 102910 0 None 33 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084673 102910 0 None 33 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
44430007 86573 0 None 17 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2F)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232476 86573 0 None 17 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2F)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718276 114802 0 None 41 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349260 114802 0 None 41 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25190573 179897 0 None 39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475308 179897 0 None 39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179053 120870 0 None -676 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581743 120870 0 None -676 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
134154039 152320 0 None -676 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@@]12C=C[C@]3(C[C@@]1(C)[C@@H](O)c1ccc(F)cc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
CHEMBL3974294 152320 0 None -676 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@@]12C=C[C@]3(C[C@@]1(C)[C@@H](O)c1ccc(F)cc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
122179053 120870 0 None -676 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581743 120870 0 None -676 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
44252838 151293 0 None -5 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3965425 151293 0 None -5 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
90306885 110463 0 None -85 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262372 110463 0 None -85 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
90306885 110463 0 None -85 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262372 110463 0 None -85 4 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
10199984 65886 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 3.2 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184547 65886 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 3.2 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
10193971 109996 0 None 15 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL324895 109996 0 None 15 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44366690 120364 0 None 12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL355931 120364 0 None 12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
44426824 85252 0 None 11 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 349 4 1 3 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccs2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228740 85252 0 None 11 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 349 4 1 3 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccs2)CC1 10.1016/j.bmcl.2007.03.061
118718268 114794 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349252 114794 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
46880030 7337 0 None 51 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1086622 7337 0 None 51 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
25129299 127646 0 None 10 4 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 2 1 3 3.9 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc2N1 nan
CHEMBL3665425 127646 0 None 10 4 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 2 1 3 3.9 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc2N1 nan
44413401 78123 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 297 3 1 2 4.3 c1cnc2[nH]cc(C3CCN(CC4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211210 78123 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 297 3 1 2 4.3 c1cnc2[nH]cc(C3CCN(CC4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44426830 143448 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL390280 143448 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2007.03.061
10134217 65929 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184698 65929 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
22562135 64518 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 351 5 1 3 3.5 CC(C)CCC(C)N1CCC(N2c3ccccc3NS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182131 64518 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 351 5 1 3 3.5 CC(C)CCC(C)N1CCC(N2c3ccccc3NS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
76313426 102858 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 484 5 1 2 7.3 N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084557 102858 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 484 5 1 2 7.3 N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44438963 91322 0 None 13 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 421 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3C=Cc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241067 91322 0 None 13 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 421 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3C=Cc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44252986 148921 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 376 4 1 2 5.2 CNC1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
CHEMBL3946074 148921 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 376 4 1 2 5.2 CNC1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
44252242 149578 0 None -6 3 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3951213 149578 0 None -6 3 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44337473 9188 0 None 7 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL110933 9188 0 None 7 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
10831914 30700 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 353 3 2 3 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3-c3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL139816 30700 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 353 3 2 3 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3-c3ccccc3)ccc2n1 10.1021/jm0002073
10150260 109943 0 None 33 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL324635 109943 0 None 33 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44391092 64322 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 8 1 5 5.4 CCc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181830 64322 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 8 1 5 5.4 CCc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44451673 168379 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL438919 168379 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
10669671 31509 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc2c(N)n1 10.1021/jm0002073
CHEMBL140580 31509 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc2c(N)n1 10.1021/jm0002073
44395410 66543 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 405 6 1 2 5.8 OC1(c2ccc(Cl)cc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL186426 66543 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 405 6 1 2 5.8 OC1(c2ccc(Cl)cc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
68629836 152725 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
CHEMBL3977691 152725 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
44437602 90209 0 None 14 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 90209 0 None 14 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
22725091 188812 0 None 2 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513171 188812 0 None 2 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44430024 153028 0 None 47 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 307 4 1 2 4.0 OC1(C2CC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL398039 153028 0 None 47 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 307 4 1 2 4.0 OC1(C2CC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
127043559 139967 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3810104 139967 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
44391104 64668 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182328 64668 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44574671 177852 0 None 9 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 452 4 1 3 6.0 Cc1ccnc(C2(O)C3CCC2CN(C(c2ccccc2Cl)c2ccccc2Cl)C3)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466082 177852 0 None 9 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 452 4 1 3 6.0 Cc1ccnc(C2(O)C3CCC2CN(C(c2ccccc2Cl)c2ccccc2Cl)C3)c1 10.1016/j.bmcl.2009.03.031
9902874 99479 0 None 24 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.0 CC(C)C1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL286411 99479 0 None 24 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.0 CC(C)C1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
44391157 64540 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182202 64540 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
118718262 114787 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 8 1 2 7.5 CCNC[C@@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349245 114787 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 8 1 2 7.5 CCNC[C@@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718299 114826 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 466 3 1 2 7.2 Fc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349284 114826 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 466 3 1 2 7.2 Fc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3810101 210519 0 None 48 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
15512233 167285 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccccc2F)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL431002 167285 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccccc2F)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
24776399 97487 0 None 9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cccc(F)c2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
CHEMBL272600 97487 0 None 9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cccc(F)c2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
68632271 142363 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 6 1 2 4.5 CNC1(c2ccccc2)CCC(Cc2ccccc2)(CN(C)C)CC1 nan
CHEMBL3893777 142363 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 6 1 2 4.5 CNC1(c2ccccc2)CCC(Cc2ccccc2)(CN(C)C)CC1 nan
90656668 110452 0 None -1096 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 501 6 2 5 4.9 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL3262091 110452 0 None -1096 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 501 6 2 5 4.9 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL263859 208840 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm990075h
59159347 127652 0 None - 1 Human 4.4 pKi = 4.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 427 3 1 5 3.7 COC(=O)c1ccc2c(c1)N(C1CCN(C3CCCCCCC3)CC1)C(=O)CC(=O)N2 nan
CHEMBL3665431 127652 0 None - 1 Human 4.4 pKi = 4.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 427 3 1 5 3.7 COC(=O)c1ccc2c(c1)N(C1CCN(C3CCCCCCC3)CC1)C(=O)CC(=O)N2 nan
10225083 165832 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL427683 165832 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
16007142 138810 0 None 97 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
CHEMBL379297 138810 0 None 97 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
9951673 85265 0 None 154 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228849 85265 0 None 154 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
9820782 142709 0 None 426 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389665 142709 0 None 426 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
118718274 114800 0 None 63 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1cccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
CHEMBL3349258 114800 0 None 63 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1cccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
44574744 188708 0 None 114 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512258 188708 0 None 114 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76309739 102831 0 None 13 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084528 102831 0 None 13 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437615 89932 0 None 67 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238637 89932 0 None 67 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437626 90178 0 None 26 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238795 90178 0 None 26 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437601 90183 0 None 7 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 90183 0 None 7 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437602 90209 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 90209 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437636 144894 0 None 31 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391422 144894 0 None 31 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10225083 165832 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 165832 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
24970041 127660 0 None 131 3 Human 8.4 pKi = 8.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
CHEMBL3665439 127660 0 None 131 3 Human 8.4 pKi = 8.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
9806799 178684 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473068 178684 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44437602 90209 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL239043 90209 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
16747695 168176 0 None 39 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 8 2 4 5.9 CC(C)S(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL437177 168176 0 None 39 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 8 2 4 5.9 CC(C)S(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44451805 95745 0 None 28 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260784 95745 0 None 28 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
53325608 56998 0 None 53 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650847 56998 0 None 53 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
53319617 57000 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650849 57000 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
53316969 57001 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650851 57001 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
11372427 178566 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
CHEMBL472125 178566 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
11188910 188843 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
CHEMBL513423 188843 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
10109140 120042 4 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 323 5 1 2 4.4 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(CCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325747 120042 4 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 323 5 1 2 4.4 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(CCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545630 120042 4 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 323 5 1 2 4.4 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(CCc2ccccc2)CC1 10.1021/ml500116x
11187225 178576 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL472168 178576 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
25190608 188643 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL511649 188643 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
57720736 120037 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 374 2 1 2 5.3 Cc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3325960 120037 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 374 2 1 2 5.3 Cc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3545625 120037 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 374 2 1 2 5.3 Cc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
52951938 77223 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088031 77223 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
53316968 56992 0 None 85 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650841 56992 0 None 85 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
52951938 77223 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088031 77223 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
44430048 87105 0 None 100 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 316 4 2 3 3.4 NCc1ccccc1C1(O)CCN(CC2CCCCCC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233535 87105 0 None 100 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 316 4 2 3 3.4 NCc1ccccc1C1(O)CCN(CC2CCCCCC2)CC1 10.1016/j.bmcl.2007.03.062
11583008 175280 4 None 213 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4585935 175280 4 None 213 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
10475466 144440 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)C1CCCC1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL391083 144440 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)C1CCCC1)CC2 10.1016/j.bmcl.2007.01.069
9885005 58419 0 None 1 4 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL168578 58419 0 None 1 4 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
44332117 107402 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
CHEMBL319307 107402 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
24776407 97281 0 None 812 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 340 2 1 2 3.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
CHEMBL271590 97281 0 None 812 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 340 2 1 2 3.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
46880114 7421 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087276 7421 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
19347346 57170 0 None 2 3 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL165885 57170 0 None 2 3 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
44451777 155844 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 531 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL406647 155844 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 531 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44451594 157749 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL408909 157749 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44252533 146661 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3928190 146661 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
44574890 178045 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 478 5 1 2 6.4 CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467497 178045 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 478 5 1 2 6.4 CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574849 188581 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 542 5 1 2 6.9 NC(=O)C1(c2ccc(Br)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511223 188581 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 542 5 1 2 6.9 NC(=O)C1(c2ccc(Br)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44394284 65841 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184381 65841 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
71624389 90025 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387200 90025 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
10454860 139331 0 None 2 2 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 3 0 7 1.0 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)[O-])C=C[C@H]4[C@@H](C2)[N+](C)(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL379928 139331 0 None 2 2 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 3 0 7 1.0 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)[O-])C=C[C@H]4[C@@H](C2)[N+](C)(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
76313422 102841 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 6 2 4 4.6 NC(=O)c1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084538 102841 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 6 2 4 4.6 NC(=O)c1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
68632816 145748 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 366 6 1 3 3.9 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CC(=O)O)CC1 nan
CHEMBL3920864 145748 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 366 6 1 3 3.9 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CC(=O)O)CC1 nan
60154189 77229 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088038 77229 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088039 77229 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
44426815 85500 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 297 4 2 3 2.7 OCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230039 85500 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 297 4 2 3 2.7 OCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44402544 69960 0 None -22 3 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 511 3 0 4 8.1 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(-c5ccccc5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL194442 69960 0 None -22 3 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 511 3 0 4 8.1 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(-c5ccccc5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
46879475 5917 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080273 5917 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44426813 86162 0 None 7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 335 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)C2CCCC2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL231608 86162 0 None 7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 335 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)C2CCCC2)CC1 10.1016/j.bmcl.2007.03.061
44402373 123470 0 None 1 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL362950 123470 0 None 1 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
9883872 119752 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL352490 119752 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
10139672 125354 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL364844 125354 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
44451724 95371 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 1 8 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnc(C)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL258897 95371 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 1 8 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnc(C)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
10154848 98708 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 349 6 0 2 4.3 CCN1C(=O)N(C2CCN(C(C)CCC(C)C)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL281322 98708 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 349 6 0 2 4.3 CCN1C(=O)N(C2CCN(C(C)CCC(C)C)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
44402415 134677 0 None -13 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 520 3 0 6 6.3 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(N5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL372244 134677 0 None -13 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 520 3 0 6 6.3 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(N5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
9880173 96838 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 321 5 1 2 3.6 CC(C)CCC(C)N1CCC(N2C(=O)N[C@@H]3CCCC[C@H]32)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL26909 96838 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 321 5 1 2 3.6 CC(C)CCC(C)N1CCC(N2C(=O)N[C@@H]3CCCC[C@H]32)CC1 10.1016/j.bmcl.2003.11.083
44391079 131955 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 407 7 1 5 5.2 Cc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL369786 131955 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 407 7 1 5 5.2 Cc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
24776409 97498 0 None 91 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 1 1 2 4.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
CHEMBL272640 97498 0 None 91 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 1 1 2 4.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
44426841 85280 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228913 85280 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2007.03.061
76327877 102854 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 0 3 6.6 CN(C)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084553 102854 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 0 3 6.6 CN(C)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
127044528 139825 0 None -83 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808415 139825 0 None -83 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
44337108 110881 0 None 6 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(Cl)c1)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL327118 110881 0 None 6 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(Cl)c1)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44252835 153643 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3985824 153643 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
46179068 125268 0 None 27 4 Human 7.4 pKi = 7.4 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 465 3 1 5 5.9 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCCC2)c1=O nan
CHEMBL3647963 125268 0 None 27 4 Human 7.4 pKi = 7.4 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 465 3 1 5 5.9 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCCC2)c1=O nan
71229805 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262089 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
71229805 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3262089 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
71229805 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262089 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
71229805 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262089 110450 0 None -295 6 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
134563691 170485 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4457077 170485 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44430025 87303 0 None 16 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 309 4 1 2 4.3 CC(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233721 87303 0 None 16 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 309 4 1 2 4.3 CC(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44252838 151293 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3965425 151293 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
10275388 162633 0 None -16 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 445 7 0 2 5.7 CCN1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL418197 162633 0 None -16 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 445 7 0 2 5.7 CCN1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
10202108 97929 1 None -16 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 417 6 1 2 5.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL27539 97929 1 None -16 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 417 6 1 2 5.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
44426844 141544 0 None 1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccc(C(c2ccc(OC)cc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
CHEMBL388122 141544 0 None 1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccc(C(c2ccc(OC)cc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
24898825 126860 0 None -13 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 426 8 0 2 6.1 CCC(=O)N(c1ccccc1)C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 nan
CHEMBL3659471 126860 0 None -13 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 426 8 0 2 6.1 CCC(=O)N(c1ccccc1)C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 nan
44366823 96543 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL266609 96543 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
46879667 5875 0 None -6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079940 5875 0 None -6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
71230446 120880 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 527 5 2 6 5.5 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(Cl)s1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581760 120880 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 527 5 2 6 5.5 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(Cl)s1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
134563650 169267 0 None 16 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439997 169267 0 None 16 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10114637 66706 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 1 3 4.9 O=S1(=O)Nc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL187183 66706 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 1 3 4.9 O=S1(=O)Nc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
90663950 106266 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 843 21 10 8 0.9 N=C(N)NCCCCC(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144465 106266 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 843 21 10 8 0.9 N=C(N)NCCCCC(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
59159323 127645 0 None 7 4 Human 6.3 pKi = 6.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 454 4 1 6 2.7 NC(=O)Cn1c(=O)c(=O)n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccccc21 nan
CHEMBL3665424 127645 0 None 7 4 Human 6.3 pKi = 6.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 454 4 1 6 2.7 NC(=O)Cn1c(=O)c(=O)n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccccc21 nan
46879476 5806 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1079561 5806 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10362733 87760 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 1 3 4.8 CN(C)c1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL234761 87760 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 1 3 4.8 CN(C)c1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
44430036 87616 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 296 4 2 3 2.6 NCc1ccccc1C1(O)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL234581 87616 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 296 4 2 3 2.6 NCc1ccccc1C1(O)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44414813 32871 0 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 379 3 1 6 1.3 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414814 32871 0 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 379 3 1 6 1.3 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL1417 32871 0 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 379 3 1 6 1.3 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44437627 168395 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 13 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)Cc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL439035 168395 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 13 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)Cc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44394344 65833 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184328 65833 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
9824313 30525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 399 5 3 5 4.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(O)cc3)ccc2n1 10.1021/jm0002073
CHEMBL139566 30525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 399 5 3 5 4.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(O)cc3)ccc2n1 10.1021/jm0002073
44391063 96266 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 497 7 2 6 5.7 Cc1ccc(Cl)c(OC(C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL264288 96266 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 497 7 2 6 5.7 Cc1ccc(Cl)c(OC(C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2004.11.049
90306863 110464 0 None -29512 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 488 5 2 6 3.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccncc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262377 110464 0 None -29512 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 488 5 2 6 3.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccncc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
44253566 143096 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 6 1 3 3.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCO)CC1 nan
CHEMBL3899856 143096 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 6 1 3 3.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCO)CC1 nan
44248917 102900 0 None 17 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1Br)C2 10.1021/jm9008218
CHEMBL3084660 102900 0 None 17 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1Br)C2 10.1021/jm9008218
76327873 102845 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2ncc(F)cc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084543 102845 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2ncc(F)cc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
127043364 139835 0 None -22 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808523 139835 0 None -22 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
10225083 165832 0 None 8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 165832 0 None 8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
25190585 178661 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL472867 178661 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179060 120878 0 None -912 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581756 120878 0 None -912 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
46879992 6128 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 4 1 5 2.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1081374 6128 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 4 1 5 2.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
46880154 5423 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 7 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076500 5423 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 7 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10315818 86924 0 None 36 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 4.8 OC1(c2cccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233323 86924 0 None 36 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 4.8 OC1(c2cccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44252682 143044 0 None -15 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3899387 143044 0 None -15 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
25190580 180046 0 None 204 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475496 180046 0 None 204 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
54580479 62304 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 419 8 1 4 4.2 c1ccc(CN2CCC[C@@H]2CNCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
CHEMBL1783821 62304 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 419 8 1 4 4.2 c1ccc(CN2CCC[C@@H]2CNCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
46880117 5421 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 382 4 1 5 2.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CC4CCC3C4)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076484 5421 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 382 4 1 5 2.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CC4CCC3C4)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337212 7638 0 None 81 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108900 7638 0 None 81 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
24894652 178450 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 348 3 0 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(=O)C2)CC1 10.1021/jm701590h
CHEMBL471301 178450 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 348 3 0 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(=O)C2)CC1 10.1021/jm701590h
44438978 145263 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccc(F)cc1)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL391703 145263 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccc(F)cc1)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2007.01.069
68632581 147807 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
CHEMBL3937167 147807 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
118662014 172289 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
CHEMBL4515245 172289 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
44181744 102885 8 None 102 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 102885 8 None 102 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
44249047 102888 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cccnc1)C2 10.1021/jm9008218
CHEMBL3084637 102888 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cccnc1)C2 10.1021/jm9008218
44426835 85260 0 None 35 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228802 85260 0 None 35 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
44426808 144183 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 323 6 1 2 4.9 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL390882 144183 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 323 6 1 2 4.9 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
118718265 114790 0 None 74 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349248 114790 0 None 74 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25190589 188545 0 None 44 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL510745 188545 0 None 44 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
46879670 5878 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079943 5878 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44437604 90210 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239045 90210 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437639 90786 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240085 90786 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437623 144635 0 None 53 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391234 144635 0 None 53 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44394487 65100 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182967 65100 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
15512241 203146 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
CHEMBL75676 203146 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
60154192 77232 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 416 5 0 4 3.7 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088043 77232 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 416 5 0 4 3.7 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
44574586 188724 0 None 102 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL512411 188724 0 None 102 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
46880089 7452 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.2 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087532 7452 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.2 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
9799433 90021 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387196 90021 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
44574790 188862 0 None 19 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 488 5 1 3 6.8 Clc1ccccc1C(c1ccccc1Cl)N1C2CCC1CC(c1ccccc1)(c1nc[nH]n1)C2 10.1016/j.bmcl.2009.03.031
CHEMBL513660 188862 0 None 19 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 488 5 1 3 6.8 Clc1ccccc1C(c1ccccc1Cl)N1C2CCC1CC(c1ccccc1)(c1nc[nH]n1)C2 10.1016/j.bmcl.2009.03.031
70686907 77018 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2086647 77018 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52952043 83170 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204349 83170 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
44253138 142673 0 None 138 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 538 9 1 8 6.1 CNc1nc(Oc2ccc(OC)cc2)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
CHEMBL3896402 142673 0 None 138 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 538 9 1 8 6.1 CNc1nc(Oc2ccc(OC)cc2)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
25190607 178446 0 None 26 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL471262 178446 0 None 26 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
9924406 113477 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 347 5 2 2 4.7 CN(C)C1(c2ccccc2)CCC(NCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326221 113477 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 347 5 2 2 4.7 CN(C)C1(c2ccccc2)CCC(NCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
118711243 120031 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 5 1 2 3.7 CN(C)C1(c2ccccc2)CCC(NC(=O)Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325880 120031 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 5 1 2 3.7 CN(C)C1(c2ccccc2)CCC(NC(=O)Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545618 120031 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 5 1 2 3.7 CN(C)C1(c2ccccc2)CCC(NC(=O)Cc2ccccc2)CC1 10.1021/ml500116x
44430049 87490 0 None 33 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 364 3 2 3 4.2 CC1(C)CCC(N2CCC(O)(c3ccccc3CN)CC2)c2ccccc21 10.1016/j.bmcl.2007.03.062
CHEMBL233957 87490 0 None 33 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 364 3 2 3 4.2 CC1(C)CCC(N2CCC(O)(c3ccccc3CN)CC2)c2ccccc21 10.1016/j.bmcl.2007.03.062
46880090 7463 0 None 14 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087658 7463 0 None 14 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10024362 79869 0 None 28 3 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 407 3 1 7 1.2 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414842 79869 0 None 28 3 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 407 3 1 7 1.2 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL214040 79869 0 None 28 3 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 407 3 1 7 1.2 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
127034023 138611 0 None 52 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3787174 138611 0 None 52 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
70690755 76283 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064130 76283 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
9954388 99065 1 None 1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283480 99065 1 None 1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
25128942 127664 0 None 21 4 Human 8.3 pKi = 8.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
CHEMBL3665443 127664 0 None 21 4 Human 8.3 pKi = 8.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
52951940 77224 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088032 77224 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951940 77224 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088032 77224 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
11451023 106725 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL316699 106725 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
127034022 138461 0 None 8 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
CHEMBL3785605 138461 0 None 8 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
10066285 191123 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL51972 191123 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
46179069 125263 0 None 117 3 Human 8.2 pKi = 8.2 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
CHEMBL3647959 125263 0 None 117 3 Human 8.2 pKi = 8.2 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
10548749 171855 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccc(Cl)cc3C1)CC2 10.1021/jm991129q
CHEMBL447779 171855 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccc(Cl)cc3C1)CC2 10.1021/jm991129q
118662309 170914 0 None 5 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 4 0 2 4.0 CCCC(=O)N1CCC2(CCC(c3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4463703 170914 0 None 5 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 4 0 2 4.0 CCCC(=O)N1CCC2(CCC(c3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
136036819 95462 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 2 8 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4n[nH]c(=O)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259291 95462 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 2 8 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4n[nH]c(=O)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44451872 95601 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 5.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259964 95601 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 5.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430081 148435 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 510 6 1 4 5.9 OC1(c2ccccc2CN2CCOCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL394222 148435 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 510 6 1 4 5.9 OC1(c2ccccc2CN2CCOCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
118718281 114807 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 465 5 1 3 6.3 Cc1cccnc1[C@@]1(CN)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349265 114807 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 465 5 1 3 6.3 Cc1cccnc1[C@@]1(CN)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718298 114825 1 None 23 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 448 3 1 2 7.1 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@]1(CNc3ccccc31)C2 10.1016/j.bmcl.2008.10.088
CHEMBL3349283 114825 1 None 23 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 448 3 1 2 7.1 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@]1(CNc3ccccc31)C2 10.1016/j.bmcl.2008.10.088
9802205 116022 0 None - 1 Human 7.3 pKi = 7.3 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 383 5 2 4 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL336238 116022 0 None - 1 Human 7.3 pKi = 7.3 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 383 5 2 4 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3)ccc2n1 10.1021/jm0002073
1222 1626 44 None -194 33 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
3396 1626 44 None -194 33 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
85 1626 44 None -194 33 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
CHEMBL46516 1626 44 None -194 33 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
DB04842 1626 44 None -194 33 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
CHEMBL265392 208889 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
10052051 66628 0 None -3162 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 510 7 1 3 5.5 CN(C)C(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL186795 66628 0 None -3162 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 510 7 1 3 5.5 CN(C)C(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
44391102 123241 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 533 7 1 7 6.6 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)n3ccnc3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL362240 123241 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 533 7 1 7 6.6 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)n3ccnc3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
44252537 153294 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3982674 153294 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
10133108 78682 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 359 2 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL2113262 78682 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 359 2 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2003.11.083
24776404 97535 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 444 3 0 2 6.2 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL272805 97535 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 444 3 0 2 6.2 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
10093682 86325 2 None 20 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 421 4 1 2 5.5 OC1(c2ccc(Br)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232067 86325 2 None 20 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 421 4 1 2 5.5 OC1(c2ccc(Br)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
24894783 186129 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 352 3 2 4 2.8 Cc1ccccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
CHEMBL488655 186129 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 352 3 2 4 2.8 Cc1ccccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
25129301 127663 0 None 239 3 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 370 2 1 4 3.3 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccnc2N1 nan
CHEMBL3665441 127663 0 None 239 3 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 370 2 1 4 3.3 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccnc2N1 nan
9969865 65402 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 4 1 3 4.0 CCCC1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL183464 65402 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 4 1 3 4.0 CCCC1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
12114744 77638 0 None 1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 469 4 1 7 2.5 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414877 77638 0 None 1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 469 4 1 7 2.5 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL209751 77638 0 None 1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 469 4 1 7 2.5 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44391067 63114 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
CHEMBL179797 63114 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
44413361 137840 0 None 16 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL377237 137840 0 None 16 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
12985907 119887 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL353608 119887 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
25128941 127654 0 None 81 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 394 3 0 6 3.4 N#CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
CHEMBL3665433 127654 0 None 81 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 394 3 0 6 3.4 N#CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
44253137 149543 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 445 7 2 7 4.3 CNc1nc(NC)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
CHEMBL3950879 149543 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 445 7 2 7 4.3 CNc1nc(NC)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
44426828 85256 0 None 51 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
CHEMBL228793 85256 0 None 51 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
25190576 189149 0 None 35 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL515901 189149 0 None 35 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
44252538 148843 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 4 1 3 4.2 CNC1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
CHEMBL3945501 148843 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 4 1 3 4.2 CNC1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
68629836 152725 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
CHEMBL3977691 152725 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
44297697 101253 0 None -30 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
CHEMBL299660 101253 0 None -30 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
10043898 85287 0 None 6 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 0 2 5.4 COC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228965 85287 0 None 6 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 0 2 5.4 COC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44402704 125855 0 None -17 3 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL365101 125855 0 None -17 3 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
24799848 97239 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
CHEMBL271341 97239 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
9924923 148140 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL393985 148140 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
118718263 114788 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 7 0 2 7.5 CN(C)C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349246 114788 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 7 0 2 7.5 CN(C)C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44413286 138522 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 325 3 1 2 5.1 c1cnc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL378633 138522 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 325 3 1 2 5.1 c1cnc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
76331525 102859 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084558 102859 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
25190581 180049 0 None 199 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475497 180049 0 None 199 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179057 120875 0 None -398 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581753 120875 0 None -398 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
122179058 120876 0 None -794 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581754 120876 0 None -794 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
25128942 127665 0 None 12 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
CHEMBL3665444 127665 0 None 12 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
22562132 167886 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 369 2 1 3 2.8 O=S1(=O)Nc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL435091 167886 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 369 2 1 3 2.8 O=S1(=O)Nc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
44252988 145593 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3919659 145593 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44413385 77288 0 None 4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 386 2 1 1 6.5 Clc1cccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
CHEMBL208862 77288 0 None 4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 386 2 1 1 6.5 Clc1cccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
25190574 188984 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514606 188984 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10286440 5141 0 None 14 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106235 5141 0 None 14 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
122179063 120881 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 493 5 2 6 4.8 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581761 120881 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 493 5 2 6 4.8 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
10172398 7636 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 5 1 2 5.0 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1F 10.1016/s0960-894x(02)00652-2
CHEMBL108894 7636 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 5 1 2 5.0 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1F 10.1016/s0960-894x(02)00652-2
118718278 114804 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 536 7 0 2 8.2 Fc1ccc(C[C@@]2(CN3CCCC3)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
CHEMBL3349262 114804 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 536 7 0 2 8.2 Fc1ccc(C[C@@]2(CN3CCCC3)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
24894431 190587 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.1 CC1(c2ccccc2)CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL518922 190587 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.1 CC1(c2ccccc2)CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
54580478 62300 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
CHEMBL1783817 62300 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
54585395 62301 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
CHEMBL1783818 62301 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
57502917 127657 0 None -1 4 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 440 3 1 6 3.3 O=c1[nH]c2ccc(N3CCOCC3)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665436 127657 0 None -1 4 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 440 3 1 6 3.3 O=c1[nH]c2ccc(N3CCOCC3)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
10384734 154424 0 None 17 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL401234 154424 0 None 17 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
10022129 85296 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 0 2 5.8 CCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL229016 85296 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 0 2 5.8 CCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44395306 66523 0 None -2570 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 463 7 1 4 5.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL186300 66523 0 None -2570 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 463 7 1 4 5.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
44252241 147664 0 None 100 3 Human 8.2 pKi = 8.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 322 4 0 2 4.5 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3935944 147664 0 None 100 3 Human 8.2 pKi = 8.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 322 4 0 2 4.5 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
16061455 102894 0 None 194 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 423 4 0 3 6.3 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccn1)C2 10.1021/jm9008218
CHEMBL3084649 102894 0 None 194 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 423 4 0 3 6.3 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccn1)C2 10.1021/jm9008218
44426840 85279 0 None 24 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228912 85279 0 None 24 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
16733371 114791 0 None 123 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 7 1 3 6.7 CCNC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349249 114791 0 None 123 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 7 1 3 6.7 CCNC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718289 114815 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 450 5 1 2 6.6 NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349273 114815 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 450 5 1 2 6.6 NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44561518 188854 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL513585 188854 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
44574743 178016 0 None 95 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467313 178016 0 None 95 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574705 178200 0 None 104 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468952 178200 0 None 104 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76324310 102835 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 5.8 Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084532 102835 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 5.8 Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
76320665 102850 0 None 51 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084549 102850 0 None 51 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
10020165 106795 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL317152 106795 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
44437617 154427 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL401248 154427 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10020165 106795 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL317152 106795 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm034249d
10385808 65796 0 None 33 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 33 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10832445 96969 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 361 2 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc3C1)CC2 10.1021/jm991129q
CHEMBL26999 96969 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 361 2 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc3C1)CC2 10.1021/jm991129q
44438974 90684 0 None 89 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1F)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239820 90684 0 None 89 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1F)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
44414829 32991 4 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
5484063 32991 4 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL1418 32991 4 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
46879539 5405 0 None 53 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1076242 5405 0 None 53 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
10788833 30818 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 5 1 4 5.6 Cc1cc(N)c2cc(N(C)C(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL139934 30818 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 5 1 4 5.6 Cc1cc(N)c2cc(N(C)C(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
71624270 90019 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387194 90019 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
53326167 56996 0 None 5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 541 6 1 6 5.7 OCC1(N2CCC(n3c(N4CC5CN(Cc6ccccc6)CC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650845 56996 0 None 5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 541 6 1 6 5.7 OCC1(N2CCC(n3c(N4CC5CN(Cc6ccccc6)CC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
24776401 158418 0 None 141 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 0 2 5.8 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL409621 158418 0 None 141 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 0 2 5.8 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL414543 211381 0 None - 1 Human 8.2 pKi = 8.2 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
25190620 178717 0 None 12 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
CHEMBL473280 178717 0 None 12 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
10504545 99025 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 469 4 0 3 5.2 C=CCN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
CHEMBL283265 99025 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 469 4 0 3 5.2 C=CCN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
9934232 91362 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL241272 91362 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
9934232 91362 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241272 91362 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
44391111 65258 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 443 7 2 6 4.6 CCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL183323 65258 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 443 7 2 6 4.6 CCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
54584439 62302 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 8 2 4 2.8 O=C(CNCc1ccccc1)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
CHEMBL1783819 62302 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 8 2 4 2.8 O=C(CNCc1ccccc1)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
118662183 171126 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 334 5 0 3 4.1 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
CHEMBL4466714 171126 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 334 5 0 3 4.1 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
44380305 59010 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 439 2 1 3 6.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL170674 59010 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 439 2 1 3 6.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
59159326 128506 0 None - 1 Human 5.2 pKi = 5.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)N(C1CCN(C3/C=C\CCCCC3)CC1)C(=O)CC(=O)N2 nan
CHEMBL3670296 128506 0 None - 1 Human 5.2 pKi = 5.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)N(C1CCN(C3/C=C\CCCCC3)CC1)C(=O)CC(=O)N2 nan
44394559 65961 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184865 65961 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
44438912 90764 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(CC1CCCCC1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240001 90764 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(CC1CCCCC1)CC2 10.1016/j.bmcl.2007.01.069
57502893 127650 0 None 4 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 1 3 4.0 CC(C)C1CCC(N2CCC(N3C(=O)CC(=O)Nc4ccccc43)CC2)CC1 nan
CHEMBL3665429 127650 0 None 4 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 1 3 4.0 CC(C)C1CCC(N2CCC(N3C(=O)CC(=O)Nc4ccccc43)CC2)CC1 nan
44426803 85498 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 1 2 5.2 OC1(c2ccccc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230033 85498 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 1 2 5.2 OC1(c2ccccc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44413362 139405 0 None 12 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 471 6 1 4 5.3 CN(C)C[C@@H](O)Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2006.03.094
CHEMBL379971 139405 0 None 12 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 471 6 1 4 5.3 CN(C)C[C@@H](O)Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2006.03.094
10314141 87784 0 None 17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 3 1 2 4.6 CC(C)(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL234771 87784 0 None 17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 3 1 2 4.6 CC(C)(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718285 114811 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2008.10.088
CHEMBL3349269 114811 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2008.10.088
46880088 7451 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087531 7451 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
122179061 120879 0 None -691 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581757 120879 0 None -691 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44253568 145149 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 4 2 2 5.1 CNC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
CHEMBL3916201 145149 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 4 2 2 5.1 CNC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
44390999 65246 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 343 4 2 5 3.3 Oc1nc2ccccc2n1C1CCN(CC(O)C2CCCCC2)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL183242 65246 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 343 4 2 5 3.3 Oc1nc2ccccc2n1C1CCN(CC(O)C2CCCCC2)CC1 10.1016/j.bmcl.2004.11.049
44402349 132906 0 None -2 3 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 450 2 1 5 6.0 Nc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL370607 132906 0 None -2 3 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 450 2 1 5 6.0 Nc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
57502892 127649 0 None 10 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 425 4 1 3 5.4 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCCCCCC3)CC2)C1=O nan
CHEMBL3665428 127649 0 None 10 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 425 4 1 3 5.4 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCCCCCC3)CC2)C1=O nan
44252533 146661 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3928190 146661 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
44394405 64221 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL181545 64221 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
25134074 127641 0 None - 1 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2c(F)cccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665420 127641 0 None - 1 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2c(F)cccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL414963 211407 0 None - 1 Mouse 6.2 pKi = 6.2 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None Cc1ccc(C[C@H](N)CNCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm990075h
10154739 96567 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 4 1 2 4.1 CCCC1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL26681 96567 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 4 1 2 4.1 CCCC1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
44252100 148592 0 None -10 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3943372 148592 0 None -10 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
44337123 109998 0 None 54 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(F)c1)c1cccc(F)c1 10.1016/s0960-894x(02)00652-2
CHEMBL324897 109998 0 None 54 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(F)c1)c1cccc(F)c1 10.1016/s0960-894x(02)00652-2
134578506 173718 0 None 58 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4550088 173718 0 None 58 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
24776412 172094 0 None 40 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 418 6 1 2 5.6 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
CHEMBL449966 172094 0 None 40 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 418 6 1 2 5.6 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
25134073 127640 0 None 2 4 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 355 2 1 4 3.4 O=c1[nH]c2ccccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665419 127640 0 None 2 4 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 355 2 1 4 3.4 O=c1[nH]c2ccccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
44339526 9220 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 403 3 1 2 5.2 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111105 9220 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 403 3 1 2 5.2 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
10252647 178636 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL472676 178636 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44413384 165790 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 6.4 Clc1cccc2c(C3CCN(CC4CCCCCCC4)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
CHEMBL427395 165790 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 6.4 Clc1cccc2c(C3CCN(CC4CCCCCCC4)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
56661555 65362 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 4 2 5 5.1 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Cl)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834415 65362 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 4 2 5 5.1 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Cl)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
118718284 114810 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 590 8 1 4 7.2 CC(=O)NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349268 114810 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 590 8 1 4 7.2 CC(=O)NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44430046 87308 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233749 87308 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.062
44426839 168247 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 387 5 2 3 4.5 O=C(O)c1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL437742 168247 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 387 5 2 3 4.5 O=C(O)c1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44574889 178043 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 507 6 2 3 5.2 NC(=O)c1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
CHEMBL467494 178043 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 507 6 2 3 5.2 NC(=O)c1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
118718295 114822 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 6 0 2 7.3 O=C1CCCN1C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349280 114822 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 6 0 2 7.3 O=C1CCCN1C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118662014 172289 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
CHEMBL4515245 172289 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
59159321 128507 0 None 173 2 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 445 3 1 5 3.6 COC(=O)C1(N2CCC(N3C(=O)CC(=O)Nc4ccc(F)cc43)CC2)CCCCCCC1 nan
CHEMBL3670297 128507 0 None 173 2 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 445 3 1 5 3.6 COC(=O)C1(N2CCC(N3C(=O)CC(=O)Nc4ccc(F)cc43)CC2)CCCCCCC1 nan
44337249 5129 0 None 6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106190 5129 0 None 6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44337460 108679 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL321462 108679 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/s0960-894x(02)00652-2
44249048 102892 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccncc1)C2 10.1021/jm9008218
CHEMBL3084642 102892 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccncc1)C2 10.1021/jm9008218
44402509 70263 0 None 1 3 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL194994 70263 0 None 1 3 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2005.03.076
44339449 8996 7 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 353 3 1 2 4.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109916 8996 7 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 353 3 1 2 4.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
9902583 97008 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 341 4 0 2 3.7 CCN1C(=O)N(C2CCN(Cc3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL27018 97008 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 341 4 0 2 3.7 CCN1C(=O)N(C2CCN(Cc3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
9845765 30995 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 397 5 2 4 5.3 Cc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
CHEMBL140103 30995 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 397 5 2 4 5.3 Cc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
44248550 102907 0 None 128 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 519 6 0 3 7.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1CN1CCCCC1)C2 10.1021/jm9008218
CHEMBL3084669 102907 0 None 128 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 519 6 0 3 7.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1CN1CCCCC1)C2 10.1021/jm9008218
118718266 114792 0 None 109 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349250 114792 0 None 109 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718279 114805 0 None 87 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349263 114805 0 None 87 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44574891 188865 0 None 30 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513667 188865 0 None 30 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44247589 102832 0 None 17 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084529 102832 0 None 17 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76327876 102849 0 None 29 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 455 4 1 3 6.1 N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084548 102849 0 None 29 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 455 4 1 3 6.1 N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44414783 141125 0 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 367 2 2 6 1.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414784 141125 0 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 367 2 2 6 1.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL385448 141125 0 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 367 2 2 6 1.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
46879716 5949 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080483 5949 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
9883872 58833 0 None 8 3 Rat 8.2 pKi = 8.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL169947 58833 0 None 8 3 Rat 8.2 pKi = 8.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
10646744 96945 0 None -2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 439 4 1 4 3.3 O=C1N(CCO)CN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL26987 96945 0 None -2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 439 4 1 4 3.3 O=C1N(CCO)CN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
10572810 99087 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283617 99087 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
44574539 177860 0 None 97 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 466 4 1 3 6.6 Cc1ccnc(C2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466126 177860 0 None 97 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 466 4 1 3 6.6 Cc1ccnc(C2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)c1 10.1016/j.bmcl.2009.03.031
60154189 77229 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088038 77229 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088039 77229 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
44253567 143952 0 None 48 2 Human 8.1 pKi = 8.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 6 1 3 3.6 CNC(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3906866 143952 0 None 48 2 Human 8.1 pKi = 8.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 6 1 3 3.6 CNC(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44574632 188705 0 None 41 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 433 6 2 3 5.5 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(CCCO)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL512247 188705 0 None 41 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 433 6 2 3 5.5 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(CCCO)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
118722880 120025 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 322 6 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325878 120025 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 322 6 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545580 120025 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 322 6 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2ccccc2)CC1 10.1021/ml500116x
10137876 124516 0 None 11 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364398 124516 0 None 11 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
11461888 4543 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 4543 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
11461888 4543 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 4543 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
10156821 177954 0 None 67 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 383 4 1 2 5.7 OC1(c2ccccc2)CC2CCCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL466846 177954 0 None 67 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 383 4 1 2 5.7 OC1(c2ccccc2)CC2CCCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
71624265 90013 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387188 90013 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
46879669 5877 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079942 5877 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44451592 95463 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259292 95463 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
118718294 114821 0 None 60 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 504 6 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@@](CN1CCCC1)(c1ccccc1)C2 10.1016/j.bmcl.2008.10.088
CHEMBL3349279 114821 0 None 60 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 504 6 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@@](CN1CCCC1)(c1ccccc1)C2 10.1016/j.bmcl.2008.10.088
45270712 193624 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 470 4 0 2 6.7 CC(=O)N1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551454 193624 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 470 4 0 2 6.7 CC(=O)N1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
10042904 206654 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL99738 206654 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
44413441 79517 0 None -2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 372 3 1 1 6.7 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2006.03.094
CHEMBL212574 79517 0 None -2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 372 3 1 1 6.7 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2006.03.094
10182346 124119 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 449 6 1 4 4.4 O=S1(=O)Nc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364147 124119 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 449 6 1 4 4.4 O=S1(=O)Nc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
44339450 109711 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 385 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL323729 109711 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 385 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
11480038 106268 0 None 35 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 900 22 10 9 -0.2 CC(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144468 106268 0 None 35 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 900 22 10 9 -0.2 CC(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
10317947 85297 0 None 20 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 385 7 0 2 6.2 CCCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL229017 85297 0 None 20 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 385 7 0 2 6.2 CCCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
76335140 102838 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 481 5 2 4 5.2 NC(=O)[C@@]1(c2ccc(O)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084535 102838 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 481 5 2 4 5.2 NC(=O)[C@@]1(c2ccc(O)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44252683 144584 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
CHEMBL3911970 144584 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
44337129 5100 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 420 7 1 3 6.3 N[C@@H](c1ccc(Oc2ccccc2)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL106043 5100 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 420 7 1 3 6.3 N[C@@H](c1ccc(Oc2ccccc2)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44252990 147858 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 389 6 1 2 5.6 CN(Cc1c[nH]c2ccccc12)CC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3937593 147858 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 389 6 1 2 5.6 CN(Cc1c[nH]c2ccccc12)CC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
118718300 114827 0 None 13 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 462 3 1 2 7.4 Cc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349285 114827 0 None 13 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 462 3 1 2 7.4 Cc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24800016 97206 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
CHEMBL271185 97206 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
44337163 5337 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL107288 5337 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
76331524 102839 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 490 5 1 4 5.4 N#Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084536 102839 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 490 5 1 4 5.4 N#Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
90306885 110463 0 None -85 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262372 110463 0 None -85 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
44402816 140158 0 None -3 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL381664 140158 0 None -3 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
134156152 150595 0 None -5 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CC(NC(=O)/C=C/c1ccccc1)C1CCC(c2cccc(F)c2)(N(C)C)CC1 nan
CHEMBL3959501 150595 0 None -5 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CC(NC(=O)/C=C/c1ccccc1)C1CCC(c2cccc(F)c2)(N(C)C)CC1 nan
90655976 110507 0 None -38 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262549 110507 0 None -38 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
44414724 32755 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 381 3 1 6 1.6 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414725 32755 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 381 3 1 6 1.6 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL1416 32755 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 381 3 1 6 1.6 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44391093 64112 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 505 8 2 6 5.4 Cc1ccc(Cl)c(OC(Cc2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL181342 64112 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 505 8 2 6 5.4 Cc1ccc(Cl)c(OC(Cc2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
9848990 188566 1 None -812 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 467 4 2 5 4.4 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 10.1021/jm401964y
CHEMBL2368861 188566 1 None -812 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 467 4 2 5 4.4 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 10.1021/jm401964y
CHEMBL511142 188566 1 None -812 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 467 4 2 5 4.4 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 10.1021/jm401964y
9848990 188566 1 None -812 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 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 10.1021/jm2003238
CHEMBL2368861 188566 1 None -812 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 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 10.1021/jm2003238
CHEMBL511142 188566 1 None -812 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 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 10.1021/jm2003238
44252682 143044 0 None -15 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3899387 143044 0 None -15 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
44337513 5110 0 None 2 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106084 5110 0 None 2 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
10413540 124983 0 None -707 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 497 7 1 4 5.5 COC(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL364625 124983 0 None -707 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 497 7 1 4 5.5 COC(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
10171862 120044 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325748 120044 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545632 120044 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCc2ccccc2)CC1 10.1021/ml500116x
44297519 100139 0 None -16 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL291901 100139 0 None -16 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
44337452 5169 0 None 75 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106366 5169 0 None 75 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
76324311 102861 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccncc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084560 102861 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccncc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
122179052 120868 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581741 120868 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44328141 96507 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 1182 31 16 15 -4.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O nan
CHEMBL266314 96507 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 1182 31 16 15 -4.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O nan
122179052 120868 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581741 120868 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
10596013 120975 0 None - 1 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 381 5 2 3 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCc3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL358306 120975 0 None - 1 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 381 5 2 3 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCc3ccccc3)ccc2n1 10.1021/jm0002073
44574672 188785 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512950 188785 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
25190597 177106 0 None 35 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL464192 177106 0 None 35 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44402586 71538 0 None 5 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL197135 71538 0 None 5 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
1692 2114 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
5311340 2114 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
CHEMBL140979 2114 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
1692 2114 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
5311340 2114 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
CHEMBL140979 2114 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
44574962 177928 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 8 1 3 6.4 COCCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466693 177928 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 8 1 3 6.4 COCCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44391155 64922 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182819 64922 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
44439001 91331 0 None 7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 407 2 1 3 4.4 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2007.01.069
CHEMBL241087 91331 0 None 7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 407 2 1 3 4.4 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2007.01.069
56664973 65355 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
CHEMBL1834409 65355 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
10646745 99056 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 439 4 0 4 3.9 COCN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
CHEMBL283432 99056 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 439 4 0 4 3.9 COCN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
11602409 138582 0 None 26 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3786899 138582 0 None 26 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
90655974 110504 0 None -8 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262546 110504 0 None -8 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
25190588 174220 0 None 28 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL456225 174220 0 None 28 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
71624388 90022 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387197 90022 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
24776397 97488 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL272601 97488 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
25134077 127644 0 None 48 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 397 2 1 4 3.8 O=c1[nH]c2ccccc2n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c1=O nan
CHEMBL3665423 127644 0 None 48 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 397 2 1 4 3.8 O=c1[nH]c2ccccc2n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c1=O nan
81689704 120872 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581750 120872 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
134134623 143964 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@@]12CC[C@]3(C[C@@]1(C)[C@@H](O)c1ccccc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
CHEMBL3907014 143964 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@@]12CC[C@]3(C[C@@]1(C)[C@@H](O)c1ccccc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
81689704 120872 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581750 120872 0 None -1995 4 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
53319616 56997 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 467 4 0 7 4.1 COC(=O)C1(N2CCC(n3c(N4CCN(C)CC4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650846 56997 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 467 4 0 7 4.1 COC(=O)C1(N2CCC(n3c(N4CCN(C)CC4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
16665915 138402 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(Cc4cccc5ccccc45)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL378458 138402 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(Cc4cccc5ccccc45)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44413301 139009 0 None 10 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 367 2 0 3 5.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
CHEMBL379657 139009 0 None 10 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 367 2 0 3 5.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
24776405 95504 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
CHEMBL259473 95504 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
15586319 120032 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 288 3 0 3 2.7 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCOCC2)CC1 10.1021/ml500116x
CHEMBL3326219 120032 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 288 3 0 3 2.7 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCOCC2)CC1 10.1021/ml500116x
CHEMBL3545620 120032 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 288 3 0 3 2.7 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCOCC2)CC1 10.1021/ml500116x
44391137 65759 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 510 7 1 6 6.1 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)N(C)C)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183918 65759 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 510 7 1 6 6.1 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)N(C)C)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
44426821 85251 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 422 5 2 3 4.6 O=C(Nc1c(F)cccc1F)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228738 85251 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 422 5 2 3 4.6 O=C(Nc1c(F)cccc1F)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
118718267 114793 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349251 114793 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
9824268 164491 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 398 5 3 5 4.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(N)cc3)ccc2n1 10.1021/jm0002073
CHEMBL422641 164491 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 398 5 3 5 4.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(N)cc3)ccc2n1 10.1021/jm0002073
44413414 137880 1 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 2 5.1 c1ccc2c(CN3CCC(c4c[nH]c5ncccc45)CC3)cccc2c1 10.1016/j.bmcl.2006.03.094
CHEMBL377402 137880 1 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 2 5.1 c1ccc2c(CN3CCC(c4c[nH]c5ncccc45)CC3)cccc2c1 10.1016/j.bmcl.2006.03.094
122179055 120873 0 None -6760 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581751 120873 0 None -6760 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
21345767 79800 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 471 4 1 7 2.8 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414801 79800 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 471 4 1 7 2.8 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL213737 79800 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 471 4 1 7 2.8 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
10178563 99032 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 391 4 0 2 4.9 CCN1C(=O)N(C2CCN(Cc3ccc4ccccc4c3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL283301 99032 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 391 4 0 2 4.9 CCN1C(=O)N(C2CCN(Cc3ccc4ccccc4c3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
44438914 91274 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccncc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240897 91274 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccncc1)CC2 10.1016/j.bmcl.2007.01.069
44339707 110141 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2cccc3ccccc23)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL325774 110141 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2cccc3ccccc23)CC1 10.1016/s0960-894x(03)00665-6
25190575 178637 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL472677 178637 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
44394375 123154 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL362160 123154 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
54581497 62308 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783827 62308 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
44391099 65593 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 429 6 2 6 4.2 Cc1ccc(Cl)c(OC(C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183603 65593 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 429 6 2 6 4.2 Cc1ccc(Cl)c(OC(C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
12114743 168238 0 None -2 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 409 3 1 7 1.5 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414785 168238 0 None -2 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 409 3 1 7 1.5 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL437682 168238 0 None -2 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 409 3 1 7 1.5 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
25190572 178889 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474091 178889 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44430016 87072 0 None 11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233493 87072 0 None 11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
10668903 34702 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 403 5 2 4 5.3 Nc1ccnc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc12 10.1021/jm0002073
CHEMBL143243 34702 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 403 5 2 4 5.3 Nc1ccnc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc12 10.1021/jm0002073
44252837 144265 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3909426 144265 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
44339463 9240 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111233 9240 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
44339463 9240 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL111233 9240 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.032
69616387 78588 0 None -5 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)CC1CC2c3ccccc3Oc3ccccc3C2O1 10.1016/j.bmcl.2005.03.076
CHEMBL2113093 78588 0 None -5 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)CC1CC2c3ccccc3Oc3ccccc3C2O1 10.1016/j.bmcl.2005.03.076
10715725 118711 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 5 2 3 5.5 Cc1ccc(CCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
CHEMBL343424 118711 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 5 2 3 5.5 Cc1ccc(CCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
118705901 112357 0 None -7943 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 490 4 2 5 4.0 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CC1CCCCC1 10.1016/j.bmc.2014.05.065
CHEMBL3309518 112357 0 None -7943 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 490 4 2 5 4.0 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CC1CCCCC1 10.1016/j.bmc.2014.05.065
44276782 98856 0 None 4 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.7 CCN1C(=O)N(C2CCN(C3CCC(C(C)C)CC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL282195 98856 0 None 4 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.7 CCN1C(=O)N(C2CCN(C3CCC(C(C)C)CC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
25190577 189109 0 None 26 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL515554 189109 0 None 26 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
25128943 127656 0 None 14 4 Human 7.1 pKi = 7.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 356 2 1 5 2.8 O=c1[nH]c2ncccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665435 127656 0 None 14 4 Human 7.1 pKi = 7.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 356 2 1 5 2.8 O=c1[nH]c2ncccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL415583 211433 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None COc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
44252837 144265 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3909426 144265 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
44249045 102887 0 None 46 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 452 5 0 3 6.9 COc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
CHEMBL3084636 102887 0 None 46 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 452 5 0 3 6.9 COc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
44249046 102906 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 421 4 0 1 7.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccc1)C2 10.1021/jm9008218
CHEMBL3084668 102906 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 421 4 0 1 7.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccc1)C2 10.1021/jm9008218
44426838 85270 0 None 13 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228858 85270 0 None 13 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44426811 161187 0 None 14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 6 1 2 5.1 CC(C)CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL413791 161187 0 None 14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 6 1 2 5.1 CC(C)CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
76327874 102846 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084544 102846 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44438965 166298 0 None 87 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL428563 166298 0 None 87 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
44438968 168423 0 None 38 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 425 4 1 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL439212 168423 0 None 38 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 425 4 1 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
46179067 125265 0 None 177 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 451 3 1 5 5.5 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCC2)c1=O nan
CHEMBL3647960 125265 0 None 177 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 451 3 1 5 5.5 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCC2)c1=O nan
52951942 83169 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204348 83169 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
60154190 77230 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 398 5 0 4 3.6 CN(C)C(=O)C(Cc1ccccc1)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088040 77230 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 398 5 0 4 3.6 CN(C)C(=O)C(Cc1ccccc1)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
11956918 120026 0 None -8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 390 3 1 3 5.0 COc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3325962 120026 0 None -8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 390 3 1 3 5.0 COc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3545583 120026 0 None -8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 390 3 1 3 5.0 COc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
134578456 171561 0 None 32 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4473045 171561 0 None 32 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44451895 95350 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL258781 95350 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430047 154200 0 None 64 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2cccc(F)c2)c2cccc(F)c2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL400036 154200 0 None 64 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2cccc(F)c2)c2cccc(F)c2)CC1 10.1016/j.bmcl.2007.03.062
129188443 168959 0 None 38 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 168959 0 None 38 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
70682351 76295 0 None 24 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064158 76295 0 None 24 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
71624268 90016 0 None -2 3 Human 8.0 pKi = 8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387191 90016 0 None -2 3 Human 8.0 pKi = 8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
44252536 152747 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
CHEMBL3977883 152747 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
24776410 97484 0 None 40 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 1 1 2 4.4 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL272592 97484 0 None 40 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 1 1 2 4.4 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
44391031 64498 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182049 64498 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44575091 188790 0 None 7 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 5.7 OC1(c2cccnc2)C2CCC1CN(C(c1ccccc1Cl)c1ccccc1Cl)C2 10.1016/j.bmcl.2009.03.031
CHEMBL512982 188790 0 None 7 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 5.7 OC1(c2cccnc2)C2CCC1CN(C(c1ccccc1Cl)c1ccccc1Cl)C2 10.1016/j.bmcl.2009.03.031
44451620 95453 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 1 9 3.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259262 95453 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 1 9 3.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430014 86906 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 399 7 1 2 6.1 CCCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL233287 86906 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 399 7 1 2 6.1 CCCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
24776413 97547 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 328 4 1 2 3.7 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3)CC2)CC1 10.1021/jm7009606
CHEMBL272896 97547 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 328 4 1 2 3.7 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3)CC2)CC1 10.1021/jm7009606
44253698 148926 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 473 7 0 7 4.4 CN(C)c1nc(N(C)C)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
CHEMBL3946171 148926 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 473 7 0 7 4.4 CN(C)c1nc(N(C)C)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
10150001 9057 0 None 5 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 5 1 2 4.9 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL110126 9057 0 None 5 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 5 1 2 4.9 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
44337351 108194 0 None 77 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL320804 108194 0 None 77 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44413314 79529 0 None 5 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 397 4 1 4 4.7 OCCn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
CHEMBL212630 79529 0 None 5 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 397 4 1 4 4.7 OCCn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
44252100 148592 0 None -10 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3943372 148592 0 None -10 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
44252537 153294 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3982674 153294 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44451647 155637 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL406409 155637 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44394529 66871 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 433 4 1 3 4.2 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(-c3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL187907 66871 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 433 4 1 3 4.2 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(-c3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
44402676 135479 0 None -2 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 449 2 0 4 6.7 Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL373174 135479 0 None -2 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 449 2 0 4 6.7 Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
122179050 120867 0 None -1230 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581740 120867 0 None -1230 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44328202 205913 0 None -1230 4 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 385 5 4 9 1.3 CC(C)c1ccccc1Nc1ncnc2c1ncn2[C@H]1OC(CO)C(O)C1O nan
CHEMBL95302 205913 0 None -1230 4 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 385 5 4 9 1.3 CC(C)c1ccccc1Nc1ncnc2c1ncn2[C@H]1OC(CO)C(O)C1O nan
122179050 120867 0 None -1230 4 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581740 120867 0 None -1230 4 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
11848225 862 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 862 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 862 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 862 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 862 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
44413232 140991 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 443 7 1 4 5.2 CN(C)C[C@@H](O)Cn1cc(C2CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2006.03.094
CHEMBL384681 140991 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 443 7 1 4 5.2 CN(C)C[C@@H](O)Cn1cc(C2CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2006.03.094
118718287 114813 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 576 7 1 4 7.2 CC(=O)NC[C@]1(c2ccc(N3CCCCC3)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349271 114813 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 576 7 1 4 7.2 CC(=O)NC[C@]1(c2ccc(N3CCCCC3)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
46917150 152493 0 None 1 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 429 5 0 4 5.2 CN(C)C1(c2ccccc2)CCC(C(=O)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
CHEMBL3975775 152493 0 None 1 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 429 5 0 4 5.2 CN(C)C1(c2ccccc2)CCC(C(=O)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
44252388 150620 0 None -2 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 4 1 2 5.3 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
CHEMBL3959625 150620 0 None -2 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 4 1 2 5.3 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
16131448 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
16131448 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1681 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1688 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
44361543 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
56947112 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
CHEMBL396460 2796 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1685 3854 0 None - 1 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15509719
23383556 178767 0 UNDEFINED 25 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL473700 178767 0 UNDEFINED 25 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190623 189111 0 UNDEFINED 204 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL515575 189111 0 UNDEFINED 204 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190602 178635 0 UNDEFINED 50 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL472669 178635 0 UNDEFINED 50 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
25190619 178716 0 UNDEFINED 123 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL473279 178716 0 UNDEFINED 123 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190622 178896 0 UNDEFINED 131 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL474096 178896 0 UNDEFINED 131 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190605 179900 0 UNDEFINED 15 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL475310 179900 0 UNDEFINED 15 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190603 189214 0 UNDEFINED 57 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL516389 189214 0 UNDEFINED 57 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
25190629 178526 0 UNDEFINED 41 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O None
CHEMBL471880 178526 0 UNDEFINED 41 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O None
25190604 188989 0 UNDEFINED 21 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL514662 188989 0 UNDEFINED 21 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190625 178528 0 UNDEFINED 37 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL471882 178528 0 UNDEFINED 37 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
25190601 180248 0 UNDEFINED 56 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL475707 180248 0 UNDEFINED 56 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190600 189053 0 UNDEFINED 75 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL515142 189053 0 UNDEFINED 75 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190618 178715 0 UNDEFINED 218 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL473278 178715 0 UNDEFINED 218 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 None
25190599 189420 0 UNDEFINED 85 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL517167 189420 0 UNDEFINED 85 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190616 179710 0 UNDEFINED 223 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL475094 179710 0 UNDEFINED 223 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190614 188965 0 UNDEFINED 37 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL514463 188965 0 UNDEFINED 37 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
25190613 189045 0 UNDEFINED 54 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL515091 189045 0 UNDEFINED 54 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 None
25190615 178711 0 UNDEFINED 42 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL473272 178711 0 UNDEFINED 42 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190606 178768 0 UNDEFINED 56 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL473701 178768 0 UNDEFINED 56 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190624 90686 0 UNDEFINED 37 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 None
CHEMBL239822 90686 0 UNDEFINED 37 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 None
25190621 178789 0 UNDEFINED 48 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL473898 178789 0 UNDEFINED 48 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 None
25190612 188970 0 UNDEFINED 47 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL514489 188970 0 UNDEFINED 47 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190617 178891 0 UNDEFINED 29 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL474092 178891 0 UNDEFINED 29 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 None
25190611 179387 0 UNDEFINED 23 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL474687 179387 0 UNDEFINED 23 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190609 179036 0 UNDEFINED 34 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 None
CHEMBL474283 179036 0 UNDEFINED 34 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 None
25190628 188572 0 UNDEFINED 7 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O None
CHEMBL511161 188572 0 UNDEFINED 7 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O None
None 214544 0 UNDEFINED -48977 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 2 2 5 1.5 C1CC1CN2CCC34C5C(=O)CCC3(C2CC6=C4C(=C(C=C6)O)O5)O None
None 215724 0 UNDEFINED -245470 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 550 4 5 7 2.2 CC1=CC=C(C=C1)C(=O)NC2CCC3(C4CC5=C6C3(C2OC6=C(C=C5)O)CCN4CC7CC7)O.C(=O)(C(=O)O)O None
None 215726 0 UNDEFINED -1071519 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 614 4 5 7 2.7 C1CC1CN2CCC34C5C(CCC3(C2CC6=C4C(=C(C=C6)O)O5)O)NC(=O)C7=CC=C(C=C7)Br.C(=O)(C(=O)O)O None
None 215727 0 UNDEFINED -2691 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 662 4 5 7 2.5 C1CC1CN2CCC34C5C(CCC3(C2CC6=C4C(=C(C=C6)O)O5)O)NC(=O)C7=CC=C(C=C7)I.C(=O)(C(=O)O)O None
None 215728 0 UNDEFINED -2691 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 592 4 5 7 3.2 CC(C)(C)C1=CC=C(C=C1)C(=O)NC2CCC3(C4CC5=C6C3(C2OC6=C(C=C5)O)CCN4CC7CC7)O.C(=O)(C(=O)O)O None
25190592 187620 0 UNDEFINED 56 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C None
CHEMBL499169 187620 0 UNDEFINED 56 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C None
25190630 178556 0 UNDEFINED 12 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O None
CHEMBL472086 178556 0 UNDEFINED 12 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O None
25190627 189188 0 UNDEFINED -1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O None
CHEMBL516187 189188 0 UNDEFINED -1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O None
25190583 178785 0 UNDEFINED 25 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL473884 178785 0 UNDEFINED 25 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190582 189174 0 UNDEFINED 34 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL516077 189174 0 UNDEFINED 34 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190610 179211 0 UNDEFINED 16 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL474485 179211 0 UNDEFINED 16 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190586 179713 0 UNDEFINED 239 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL475096 179713 0 UNDEFINED 239 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190593 189136 0 UNDEFINED 77 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL515829 189136 0 UNDEFINED 77 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
9937777 174775 0 UNDEFINED 114 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL457451 174775 0 UNDEFINED 114 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190598 90844 0 UNDEFINED 12 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL240215 90844 0 UNDEFINED 12 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
10323169 178792 0 UNDEFINED 6 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL473904 178792 0 UNDEFINED 6 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
25190587 190165 0 UNDEFINED 181 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL518325 190165 0 UNDEFINED 181 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190594 174679 0 UNDEFINED 87 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL457244 174679 0 UNDEFINED 87 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190579 189031 0 UNDEFINED 3 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL514965 189031 0 UNDEFINED 3 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
15541261 91131 0 UNDEFINED 6 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL240657 91131 0 UNDEFINED 6 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
25190578 179414 0 UNDEFINED 5 4 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL474708 179414 0 UNDEFINED 5 4 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
25190584 189164 0 UNDEFINED 27 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL516024 189164 0 UNDEFINED 27 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190596 177105 0 UNDEFINED 19 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL464191 177105 0 UNDEFINED 19 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190590 176211 0 UNDEFINED 91 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL460636 176211 0 UNDEFINED 91 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190626 188573 0 UNDEFINED 38 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 None
CHEMBL511162 188573 0 UNDEFINED 38 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 None
25190591 189476 0 UNDEFINED 263 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL517265 189476 0 UNDEFINED 263 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190595 187760 0 UNDEFINED 70 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL501088 187760 0 UNDEFINED 70 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
10158555 188506 0 UNDEFINED 4 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL510201 188506 0 UNDEFINED 4 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
25190573 179897 0 UNDEFINED 39 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL475308 179897 0 UNDEFINED 39 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
9806799 178684 0 UNDEFINED 141 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL473068 178684 0 UNDEFINED 141 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
None 215725 0 UNDEFINED -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 604 4 5 7 2.9 C1CC1CN2CCC34C5C(CCC3(C2CC6=C4C(=C(C=C6)O)O5)O)NC(=O)C7=CC=C(C=C7)C(F)(F)F.C(=O)(C(=O)O)O None
25190608 188643 0 UNDEFINED 3 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL511649 188643 0 UNDEFINED 3 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190585 178661 0 UNDEFINED -1 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL472867 178661 0 UNDEFINED -1 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190580 180046 0 UNDEFINED 204 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL475496 180046 0 UNDEFINED 204 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190589 188545 0 UNDEFINED 44 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL510745 188545 0 UNDEFINED 44 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190607 178446 0 UNDEFINED 26 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL471262 178446 0 UNDEFINED 26 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
1222 1626 44 UNDEFINED -194 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1626 44 UNDEFINED -194 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1626 44 UNDEFINED -194 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1626 44 UNDEFINED -194 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1626 44 UNDEFINED -194 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25190576 189149 0 UNDEFINED 35 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL515901 189149 0 UNDEFINED 35 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
25190581 180049 0 UNDEFINED 199 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL475497 180049 0 UNDEFINED 199 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190574 188984 0 UNDEFINED 13 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL514606 188984 0 UNDEFINED 13 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
1222 1626 44 None -194 33 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1626 44 None -194 33 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1626 44 None -194 33 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1626 44 None -194 33 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1626 44 None -194 33 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25190620 178717 0 UNDEFINED 12 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C None
CHEMBL473280 178717 0 UNDEFINED 12 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C None
9934232 91362 0 UNDEFINED 407 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL241272 91362 0 UNDEFINED 407 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
10252647 178636 0 UNDEFINED 8 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL472676 178636 0 UNDEFINED 8 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
3033050 214217 0 None -5 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
Drug Central 467 4 2 5 4.4 CC(C)(C)C(C)(C1CC23CCC1(C4C25CCN(C3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)O None
1627 2546 18 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
1845 2546 18 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
5288826 2546 18 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
CHEMBL70 2546 18 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
DB00295 2546 18 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
25190597 177106 0 UNDEFINED 35 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL464192 177106 0 UNDEFINED 35 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190588 174220 0 UNDEFINED 28 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL456225 174220 0 UNDEFINED 28 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190575 178637 0 UNDEFINED 7 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL472677 178637 0 UNDEFINED 7 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
25190572 178889 0 UNDEFINED 6 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL474091 178889 0 UNDEFINED 6 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
25190577 189109 0 UNDEFINED 26 3 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL515554 189109 0 UNDEFINED 26 3 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
12419 2429 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
24800108 2429 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
CHEMBL481512 2429 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
49843739 3598 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
8867 3598 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
CHEMBL3262554 3598 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
11597355 3485 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8869 3485 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8870 505 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
91938095 505 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
CHEMBL3613442 505 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
8868 3478 27 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3478 27 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3478 27 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
11848225 862 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 862 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 862 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 862 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 862 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
11848225 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 862 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8868 3478 27 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3478 27 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3478 27 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
8868 3478 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3478 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3478 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
52914971 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
52914971 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
9462 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
9462 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
CHEMBL3304244 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
CHEMBL3304244 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
DB16048 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
DB16048 2365 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
16131448 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
16131448 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
16131448 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1681 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1681 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1681 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1688 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1688 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1688 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
44361543 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
44361543 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
44361543 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
56947112 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
56947112 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
56947112 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
CHEMBL396460 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL396460 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL396460 2796 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1694 3853 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
25081457 3853 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1682 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1682 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1682 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1682 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
6324645 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
6324645 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
6324645 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
6324645 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
CHEMBL384755 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL384755 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL384755 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL384755 2799 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
8865 3175 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24903280
1686 3012 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1686 3012 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15743186
50922685 723 0 None -5 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 481 6 2 5 4.8 CO[C@]12CC[C@]3(C[C@@H]1[C@@](C(CC)(C)C)(O)C)[C@@]14[C@H]2Oc2c4c(C[C@H]3N(CC1)CC1CC1)ccc2O 21177476
9294 723 0 None -5 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 481 6 2 5 4.8 CO[C@]12CC[C@]3(C[C@@H]1[C@@](C(CC)(C)C)(O)C)[C@@]14[C@H]2Oc2c4c(C[C@H]3N(CC1)CC1CC1)ccc2O 21177476
1691 2067 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
5311194 2067 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
CHEMBL357076 2067 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
1679 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1679 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
9963005 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL437723 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
132427684 506 0 None - 1 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 5 1 3 3.9 CNC(=O)CC1C(=O)N(c2c1cccc2)C1CCN(CC1)[C@@H]1CC[C@@H](CC1)C(C)C 29232769
9747 506 0 None - 1 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 5 1 3 3.9 CNC(=O)CC1C(=O)N(c2c1cccc2)C1CCN(CC1)[C@@H]1CC[C@@H](CC1)C(C)C 29232769
10047612 3460 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
10047612 3460 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1693 3460 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
1693 3460 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
CHEMBL559569 3460 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
CHEMBL559569 3460 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1684 3298 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
1684 3298 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
9844019 3298 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
9844019 3298 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
CHEMBL2088034 3298 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
CHEMBL2088034 3298 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
1680 267 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1680 267 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
15512229 3321 0 None 1 8 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
8864 3321 0 None 1 8 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
CHEMBL355202 3321 0 None 1 8 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
10296561 1024 20 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
7361 1024 20 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
CHEMBL201945 1024 20 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
1651 2669 22 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
4673 2669 22 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
6445230 2669 22 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
CHEMBL267495 2669 22 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
DB13471 2669 22 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
1683 2800 0 None - 1 Human 10.4 pKi None 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1696 2990 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
5311338 2990 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
1692 2114 23 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
5311340 2114 23 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
CHEMBL140979 2114 23 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
1695 2819 0 None - 1 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1679 266 21 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 266 21 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 266 21 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1680 267 0 None -2 2 Mouse 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1690 1599 0 None - 1 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
16131448 2796 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2796 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2796 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2796 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2796 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2796 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
16143911 464 14 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
1689 464 14 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
CHEMBL505874 464 14 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863