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 183898 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 183898 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 3899 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 3899 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 3899 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 208795 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 208795 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 210609 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 161829 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 161829 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 159816 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 159816 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 97835 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 97835 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 97835 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 212728 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 210501 8 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 210151 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 210640 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 96472 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 96472 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 212979 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 212549 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 208788 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 213359 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 169381 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 169381 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 2832 18 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 2832 18 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 2832 18 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 208789 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 208789 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2457 29 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 2457 29 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 2457 29 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 161829 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 161829 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 210556 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 183898 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 183898 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 2832 18 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 2832 18 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 2832 18 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 3899 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 3899 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 3899 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 213503 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 208793 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 208793 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 3899 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 3899 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 3899 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 208494 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 159816 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 159816 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 213131 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 2832 18 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 2832 18 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 2832 18 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 214534 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 208795 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 213442 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 169381 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 169381 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 161829 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 161829 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 466 16 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 466 16 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 466 16 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 215570 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 466 16 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 466 16 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 466 16 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2832 18 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 2832 18 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 2832 18 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 159816 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 159816 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 214190 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 183772 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 183772 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 120539 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 120539 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 120539 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 215712 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 215720 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 191185 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 191185 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 212572 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 208493 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 183899 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 183899 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 183920 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 183920 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 188346 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 188346 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 77565 26 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 77565 26 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 214276 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 210609 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 213716 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 214221 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 214668 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 215383 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 214162 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 210511 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 90440 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 90440 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 214421 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 178553 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 178553 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 90429 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 90429 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 213887 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 214157 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 215659 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2832 18 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 2832 18 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 2832 18 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 103290 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 103290 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2832 18 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 2832 18 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 2832 18 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 120534 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 120534 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 120534 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 120534 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 65676 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 65676 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 214594 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 213887 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 143228 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 143228 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 189141 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 189141 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 189141 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 169821 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 169821 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 85698 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 85698 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 108524 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 108524 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 208383 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 208383 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 214504 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 215634 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 66112 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 66112 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 3521 31 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 3521 31 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 3521 31 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 57278 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 57278 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 213747 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 213685 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 120457 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 120457 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 212404 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 268 24 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 268 24 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 268 24 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 120532 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 120532 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 120532 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 174194 3 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 174194 3 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 77566 32 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 77566 32 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 215068 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 110982 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 110982 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 115288 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 115288 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 90439 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 90439 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 115289 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 115289 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 212404 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 183921 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 183921 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 215006 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 168747 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 168747 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 56398 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 56398 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 210621 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 14088 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 14088 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 14088 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 178763 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 178763 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 90433 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 90433 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 176382 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 176382 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 176382 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 66112 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 66112 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 56398 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 56398 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 178525 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 178525 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 121369 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 121369 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 103320 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 103320 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 144430 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 144430 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 144430 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 210150 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 210150 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 121373 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 121373 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 189141 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 189141 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 189141 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 215603 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 14147 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 14147 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 14147 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 212404 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 99511 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 99511 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 214724 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 174529 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 174529 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 115278 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 115278 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 213644 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 121658 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 121658 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 121658 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 66157 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 66157 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 178412 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 178412 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 178604 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 178604 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 107195 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 107195 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 210727 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 212478 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 66125 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 66125 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 169513 3 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 169513 3 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 121380 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 121380 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 66133 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 66133 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 189253 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 189253 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 123658 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 123658 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 125862 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 125862 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 57281 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 57281 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 155376 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 155376 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 212496 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 215402 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 108718 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 108718 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 108718 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 108718 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 176052 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 176052 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 95612 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 95612 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 103311 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 103311 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 214218 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 95325 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 95325 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 144430 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 144430 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 144430 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 214758 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 4377 16 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 4377 16 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 214174 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 210609 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 183771 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 183771 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 214307 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 214068 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 214731 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 103373 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 103373 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 195233 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 195233 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 196111 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 196111 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 196161 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 196161 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 103293 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 103293 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 14144 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 14144 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 14144 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 4377 16 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 4377 16 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 120536 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 120536 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 120536 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 66181 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 66181 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 121661 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 121661 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 121661 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 3337 21 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 3337 21 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 3337 21 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 110977 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 110977 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 212546 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 66950 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 66950 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 214263 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 212316 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 85690 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 85690 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 66643 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 66643 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 142064 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 142064 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 142064 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 142064 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 57275 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 57275 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 97692 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 97692 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 168779 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 168779 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 210150 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 210150 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 121379 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 121379 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 121383 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 121383 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 212546 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 213373 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 65674 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 65674 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 214925 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 176610 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 176610 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 176610 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 213304 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 213177 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 210530 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 85681 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 85681 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 215482 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 77566 32 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 77566 32 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 163298 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 163298 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 210670 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 90428 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 90428 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 215472 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 103291 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 103291 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 115304 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 115304 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 86804 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 86804 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 86804 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 155415 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 155415 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 110980 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 110980 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 79720 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 79720 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 173037 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 173037 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 103346 9 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 103346 9 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 4594 3 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 4594 3 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 4594 3 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 4594 3 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 212564 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 142064 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 142064 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 142064 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 142064 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 212252 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 212454 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 213884 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 208792 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 208792 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 183941 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 183941 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 215709 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 215657 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 215719 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 14146 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 14146 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 14146 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 214615 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 208791 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 2709 9 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 2709 9 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 2709 9 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 2709 9 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 212594 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 213979 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 208794 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 208794 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 214703 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 90436 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 90436 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 66246 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 66246 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 210752 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 210752 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 210630 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 166597 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 166597 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 3629 40 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 3629 40 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 3629 40 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 214176 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 125023 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 125023 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 142064 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 142064 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 142064 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 142064 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 121375 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 121375 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 66232 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 66232 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 65416 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 65416 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 171268 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 171268 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 178524 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 178524 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 208790 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 208790 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 57284 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 57284 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 215316 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 66112 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 66112 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 57282 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 57282 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 57517 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 57517 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 3360 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 3360 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 3360 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 2832 18 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 2832 18 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 2832 18 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 214104 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 208791 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 214758 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 214172 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 208492 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 213903 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 212456 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 3899 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 3899 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 3899 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 161018 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 161018 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 99142 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 99142 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 214204 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 110978 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 110978 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 209385 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 121368 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 121368 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 139328 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 139328 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 121660 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 121660 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 121660 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 120526 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 120526 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 120526 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 212568 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 103294 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 103294 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 168690 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 168690 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 174276 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 174276 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 121659 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 121659 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 121659 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 90434 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 90434 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 97451 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 97451 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 161300 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 161300 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 161300 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 173125 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 173125 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 188816 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 188816 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 214259 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 215257 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 115303 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 115303 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 64537 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 64537 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 66149 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 66149 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 191274 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 191274 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 214146 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 214158 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 214158 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 215558 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 189299 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 189299 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 189360 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 189360 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 215558 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 110979 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 110979 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 99079 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 99079 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 97483 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 97483 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 110976 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 110976 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 57283 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 57283 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 214279 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 171038 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 171038 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 178577 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 178577 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 175144 3 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 175144 3 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 90435 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 90435 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 86804 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 86804 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 86804 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 215005 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 213080 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 79914 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 79914 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 66278 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 66278 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 215342 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 172113 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 172113 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 2832 18 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 2832 18 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 2832 18 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 189300 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 189300 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 191837 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 191837 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 90438 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 90438 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 112558 11 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 112558 11 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 112558 11 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 214254 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 213887 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 213373 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 178485 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 178485 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 103295 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 103295 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 209515 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 214379 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 213168 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 169809 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 169809 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 214725 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 215329 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 174614 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 174614 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 212780 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 121371 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 121371 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 166380 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 166380 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 2832 18 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 2832 18 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 2832 18 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 110984 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 110984 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 170985 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 170985 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 107874 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 107874 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 161300 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 161300 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 161300 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 189283 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 189283 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 66943 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 66943 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 65671 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 65671 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 99637 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 99637 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 213665 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 90437 1 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 90437 1 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 57276 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 57276 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 209507 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 110981 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 110981 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 90432 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 90432 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 90430 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 90430 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 212457 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 110975 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 110975 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 214751 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 214155 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 103313 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 103313 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 98243 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 98243 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 215650 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 158799 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 158799 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 158799 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 215581 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 57277 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 57277 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 214929 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 178411 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 178411 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 4418 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 4418 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 213887 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 14145 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 14145 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 14145 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 90441 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 90441 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 173931 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 173931 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 97456 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 97456 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 209385 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 74024 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 74024 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 1039 26 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 1039 26 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 1039 26 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 178482 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 178482 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 178482 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 178482 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 188793 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 188793 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 178571 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 178571 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 194898 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 194898 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 195736 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 195736 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 187493 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 187493 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 187493 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 187493 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 96656 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 96656 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 96656 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 96656 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 178686 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 178686 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 178686 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 178686 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 178457 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 178457 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 178436 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 178436 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 195752 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 195752 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 178689 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 178689 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 178432 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 178432 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 178633 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 178633 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 178691 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 178691 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 189363 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 189363 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 178443 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 178443 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 178542 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 178542 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 2094 23 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 2094 23 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 2094 23 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 185743 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 185743 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 178567 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 178567 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 96655 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 96655 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 145494 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 145494 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 189430 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 189430 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 91724 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 91724 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 6005 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 6005 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 91768 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 91768 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 154954 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 154954 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 65095 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 65095 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 76634 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 76634 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 62576 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 62576 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 189462 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 189462 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 73632 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 73632 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 76622 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 76622 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 6009 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 6009 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 56402 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 56402 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 56402 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 187215 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 187215 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 186285 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 186285 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 76636 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 76636 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 56402 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 56402 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 56402 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 91203 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 91203 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 138978 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 138978 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 90348 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 90348 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 145155 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 145155 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 64445 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 64445 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 91868 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 91868 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 195020 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 195020 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 65580 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 65580 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 76633 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 76633 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 96187 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 96187 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 122598 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 122598 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 122598 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 122598 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 13990 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 13990 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 13990 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 63429 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 63429 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 170641 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 170641 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 6153 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 6153 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 13998 4 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 13998 4 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 13998 4 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 64856 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 64856 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 90315 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 90315 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 145690 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 145690 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 155672 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 155672 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 65541 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 65541 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 5937 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 5937 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 189356 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 189356 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 79493 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 79493 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 178685 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 178685 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 196217 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 196217 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 187703 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 187703 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 196168 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 196168 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 196678 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 196678 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 178611 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 178611 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 196038 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 196038 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 196405 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 196405 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 96657 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 96657 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 6011 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 6011 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 178709 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 178709 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 158271 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 158271 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 37971 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 37971 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 38171 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 38171 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 147608 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 147608 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 5462 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 5462 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 95867 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 95867 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 95867 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 95867 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 138974 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 138974 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 187474 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 187474 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 78084 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 78084 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 138992 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 138992 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 76627 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 76627 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 138639 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 138639 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 90625 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 90625 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 65238 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 65238 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 123287 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 123287 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 139100 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 139100 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 90599 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 90599 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 186303 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 186303 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 193218 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 193218 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 96189 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 96189 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 5938 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 5938 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 139009 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 139009 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 13991 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 13991 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 13991 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 78680 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 78680 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 156974 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 156974 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 156974 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 156974 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 189151 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 189151 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 195247 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 195247 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 96649 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 96649 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 145493 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 145493 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 56400 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 56400 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 56400 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 56400 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 56400 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 56400 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 90598 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 90598 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 91199 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 91199 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 5841 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 5841 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 138924 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 138924 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 146866 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 146866 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 166372 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 166372 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 178442 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 178442 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 166372 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 166372 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 96188 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 96188 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 56399 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 56399 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 56399 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 56399 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 56399 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 56399 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 145494 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 145494 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 178713 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 178713 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 74324 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 74324 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 178712 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 178712 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 179161 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 179161 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 195612 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 195612 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 196057 2 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 196057 2 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 187581 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 187581 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 90597 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 90597 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 178479 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 178479 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 148631 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 148631 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 76635 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 76635 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 133514 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 133514 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 77761 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 77761 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 166372 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 166372 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 91769 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 91769 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 90859 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 90859 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 76632 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 76632 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 5455 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 5455 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 139243 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 139243 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 178598 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 178598 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 187475 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 187475 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 76624 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 76624 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 189419 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 189419 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 5836 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 5836 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 178418 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 178418 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 196500 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 196500 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 2094 23 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 2094 23 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 2094 23 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 189221 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 189221 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 65433 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 65433 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 6152 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 6152 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 138991 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 138991 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 145710 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 145710 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 90314 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 90314 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 139054 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 139054 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 6010 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 6010 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 193342 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 193342 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 178478 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 178478 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 195222 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 195222 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 90625 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 90625 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 56401 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 56401 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 77908 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 77908 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 166372 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 166372 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 139129 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 139129 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 5935 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 5935 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 95929 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 95929 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 178572 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 178572 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 179131 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 179131 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 5868 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 5868 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 178492 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 178492 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 56403 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 56403 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 56403 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 72649 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 72649 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 56403 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 56403 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 56403 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 195741 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 195741 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 145494 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 145494 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 56401 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 56401 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 145537 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 145537 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 90625 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 90625 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 95763 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 95763 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 64984 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 64984 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 145414 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 145414 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 161696 1 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 161696 1 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 178431 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 178431 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 96409 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 96409 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 90599 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 90599 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 90594 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 90594 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 139318 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 139318 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 179141 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 179141 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 95762 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 95762 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 6006 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 6006 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 196167 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 196167 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 91202 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 91202 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 90626 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 90626 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 96645 1 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 96645 1 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 165867 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 165867 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 129643 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 129643 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 91201 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 91201 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 62621 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 62621 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 210151 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 210151 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 210151 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 56403 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 56403 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 56403 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 62621 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 62621 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 140341 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 140341 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 210754 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 210754 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 140343 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 140343 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 210754 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 1039 26 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 1039 26 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 1039 26 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 140485 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 140485 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 210754 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 140353 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 140353 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 9764 3 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 9764 3 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 109638 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 109638 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 9306 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 9306 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 9334 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 9334 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 8651 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 8651 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 110570 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 110570 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 9312 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 9312 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 14144 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 14144 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 14144 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 8696 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 8696 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 108817 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 108817 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 9647 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 9647 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 3823 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 3823 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 3823 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 93116 34 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 93116 34 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 2457 29 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 2457 29 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 2457 29 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 3337 21 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 3337 21 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 3337 21 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 3051 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 268 24 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 268 24 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 268 24 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 3528 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 3528 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 3641 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 3641 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 3641 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 3360 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 3360 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 3360 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 3521 31 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 3521 31 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 3521 31 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 3214 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 269 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
3917 3899 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
3917 3899 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
44430609 3899 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
44430609 3899 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
CHEMBL409969 3899 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
CHEMBL409969 3899 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
16131448 2829 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2829 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2829 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2829 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2829 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2829 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1691 2094 23 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 2094 23 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 2094 23 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 1039 26 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 1039 26 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 1039 26 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 1039 26 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 1039 26 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 1039 26 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 2806 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 2806 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 213115 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 161829 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 161829 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 210656 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 182031 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 182031 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 212685 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 159816 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 159816 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 213181 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 169381 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 169381 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 210582 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 182003 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 182003 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 183492 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 183492 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 174046 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 174046 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 210609 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 161018 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 161018 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 183302 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 183302 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 180883 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 180883 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 212832 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 180196 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 180196 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 180010 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 180010 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 182703 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 182703 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 213751 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 183374 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 183374 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 210556 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 96472 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 96472 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 213169 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 181820 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 181820 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 212606 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 182575 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 182575 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 182860 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 182860 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 172237 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 172237 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 179393 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 179393 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 210640 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 2832 18 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 2832 18 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 2832 18 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 212527 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 213821 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 180457 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 180457 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 180296 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 180296 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 180007 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 180007 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 180117 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 180117 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 181366 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 181366 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 180296 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 180296 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 212972 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 181820 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 181820 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 181791 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 181791 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 210394 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 180117 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 180117 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 210396 19 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 181414 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 181414 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 183898 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 183898 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 181854 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 181854 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 210394 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 183374 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 183374 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 180179 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 180179 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 180413 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 180413 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 182003 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 182003 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 182305 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 182305 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 4377 16 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 4377 16 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 181175 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 181175 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 179675 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 179675 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 180196 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 180196 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 181414 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 181414 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 180657 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 180657 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 180718 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 180718 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 179937 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 179937 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 183492 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 183492 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 183898 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 183898 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 38021 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 38021 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 183027 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 183027 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 180072 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 180072 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 181175 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 181175 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 182910 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 182910 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 181366 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 181366 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 183126 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 183126 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 182703 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 182703 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 182910 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 182910 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 180883 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 180883 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 182575 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 182575 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 183302 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 183302 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 161253 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 161253 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 67726 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 67726 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 181501 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 181501 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 180007 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 180007 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 179766 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 179766 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 180950 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 180950 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 180718 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 180718 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 213114 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 180457 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 180457 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 213044 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 173332 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 173332 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 179651 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 179651 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 181791 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 181791 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 180179 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 180179 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 181105 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 181105 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 179651 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 179651 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 212606 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 213131 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 213664 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 180950 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 180950 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 213080 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 99214 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 99214 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 2832 18 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 2832 18 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 2832 18 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 213116 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 180413 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 180413 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 180010 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 180010 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 182860 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 182860 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 183203 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 183203 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 182031 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 182031 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 182305 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 182305 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 210396 19 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 179766 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 179766 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 183203 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 183203 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 212972 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 179393 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 179393 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 180657 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 180657 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 183027 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 183027 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 101833 21 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 101833 21 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 181854 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 181854 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 182804 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 182804 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 183102 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 183102 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 183102 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 183102 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 181501 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 181501 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 179610 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 179610 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 179610 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 179610 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 175839 5 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 175839 5 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 179675 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 179675 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 2832 18 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 2832 18 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 2832 18 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 212795 17 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 180072 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 180072 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 182804 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 182804 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 183126 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 183126 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 179937 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 179937 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 213495 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 213333 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 181105 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 181105 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 115105 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 115105 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 115105 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 213129 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 115107 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 115107 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 169328 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 169328 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 213903 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 215570 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 466 16 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 466 16 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 466 16 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 214190 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 466 16 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 466 16 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 466 16 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 74024 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 74024 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 215712 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 215720 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 1039 26 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 1039 26 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 1039 26 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 214534 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 210640 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 215709 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 215657 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 215719 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 214104 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 2832 18 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 2832 18 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 2832 18 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 214146 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 214158 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 214172 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 214158 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 214174 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 212594 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 214162 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 178482 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 178482 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 178482 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 178482 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 213716 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 214068 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 176628 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 176628 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 176628 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 97692 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 97692 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 268 24 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 268 24 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 268 24 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 161568 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 161568 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 268 24 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 268 24 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 268 24 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 178611 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 178611 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 178542 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 178542 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 178542 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 178542 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 210752 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 194898 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 194898 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 214155 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 161543 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 161543 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 178691 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 178691 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 214176 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 215634 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 268 24 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 268 24 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 268 24 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 178571 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 178571 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 187703 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 187703 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 189363 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 189363 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 214157 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 215581 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 215603 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 96656 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 96656 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 96656 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 96656 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 212404 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 115106 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 115106 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 178443 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 178443 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 195752 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 195752 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 188793 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 188793 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 196168 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 196168 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 215659 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 115107 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 115107 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 178436 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 178436 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 155415 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 155415 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 96655 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 96655 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 178572 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 178572 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 166597 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 166597 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 178633 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 178633 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 13991 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 13991 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 13991 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 161696 1 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 161696 1 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 96649 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 96649 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 72122 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 72122 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 168410 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 168410 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 135983 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 135983 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 140596 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 140596 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 166039 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 166039 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 72270 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 72270 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 135178 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 135178 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 135336 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 135336 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 140868 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 140868 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 72818 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 72818 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 168626 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 168626 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 135234 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 135234 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 132988 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 132988 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 187215 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 187215 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 196361 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 196361 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 212510 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 60547 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 60547 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 60905 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 60905 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 133493 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 133493 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 60885 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 60885 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 60919 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 60919 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 72649 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 72649 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 74409 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 74409 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 195773 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 195773 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 133417 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 133417 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 135182 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 135182 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 96650 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 96650 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 77343 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 77343 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 60907 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 60907 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 212564 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 187501 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 187501 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 215650 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 195827 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 195827 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 72863 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 72863 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 140335 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 140335 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 141283 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 141283 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 72946 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 72946 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 117209 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 117209 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 95612 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 95612 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 97456 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 97456 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 96670 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 96670 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 155626 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 155626 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 78162 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 78162 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 60900 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 60900 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 60916 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 60916 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 60901 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 60901 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 95763 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 95763 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 195020 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 195020 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 195565 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 195565 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 155362 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 155362 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 72469 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 72469 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 178514 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 178514 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 193194 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 193194 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 72811 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 72811 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 133804 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 133804 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 79482 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 79482 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 60918 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 60918 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 60902 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 60902 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 60912 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 60912 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 178598 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 178598 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 97451 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 97451 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 117207 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 117207 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 195503 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 195503 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 196638 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 196638 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 196679 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 196679 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 117206 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 117206 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 95867 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 95867 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 96645 1 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 96645 1 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 196515 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 196515 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 95867 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 95867 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 73900 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 73900 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 117216 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 117216 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 193218 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 193218 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 136016 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 136016 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 95993 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 95993 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 60903 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 60903 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 60898 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 60898 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 10017 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 10017 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 196601 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 196601 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 9898 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 9898 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 178418 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 178418 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 195736 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 195736 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 95762 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 95762 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 178567 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 178567 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 215558 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 215558 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 115105 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 115105 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 115105 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 178457 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 178457 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 213979 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 2094 23 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 2094 23 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 2094 23 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 2094 23 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 2094 23 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 2094 23 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 13990 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 13990 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 13990 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 13998 4 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 13998 4 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 13998 4 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 2094 23 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 2094 23 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 2094 23 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 178686 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 178686 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 178686 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 178686 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 178689 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 178689 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 187493 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 187493 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 187493 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 187493 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 168690 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 168690 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 158271 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 158271 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 101833 21 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 101833 21 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 101833 21 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 101833 21 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 196264 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 196264 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 60914 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 60914 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 60920 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 60920 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 60899 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 60899 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 74173 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 74173 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 178431 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 178431 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 97483 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 97483 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 168869 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 168869 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 195908 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 195908 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 78032 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 78032 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 60917 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 60917 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 213905 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 178403 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 178403 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 3122 18 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 3122 18 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 3122 18 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 72051 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 72051 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 96188 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 96188 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 172726 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 172726 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 74016 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 74016 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 78991 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 78991 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 74372 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 74372 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 156739 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 156739 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 140604 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 140604 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 10033 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 10033 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 60915 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 60915 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 60878 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 60878 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 170250 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 170250 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 117210 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 117210 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 195515 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 195515 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 168294 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 168294 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 189229 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 189229 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 178478 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 178478 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 187476 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 187476 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 210717 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 72501 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 72501 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 189347 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 189347 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 189347 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 189347 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 196075 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 196075 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 60894 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 60894 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 163999 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 163999 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 140271 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 140271 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 73642 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 73642 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 157635 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 157635 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 159429 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 159429 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 213884 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 213644 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 196405 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 196405 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 196678 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 196678 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 95325 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 95325 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 117211 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 117211 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 140552 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 140552 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 2141 29 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 2141 29 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 2141 29 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 60892 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 60892 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 133574 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 133574 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 60910 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 60910 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 60897 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 60897 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 157228 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 157228 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 60893 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 60893 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 133574 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 133574 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 157499 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 157499 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 70240 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 70240 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 60895 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 60895 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 72345 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 72345 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 96644 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 96644 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 196039 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 196039 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 187505 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 187505 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 196088 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 196088 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 74386 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 74386 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 117202 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 117202 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 73909 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 73909 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 111328 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 111328 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 60881 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 60881 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 72164 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 72164 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 166140 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 166140 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 187475 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 187475 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 192702 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 192702 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 73910 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 73910 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 141316 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 141316 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 168766 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 168766 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 117214 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 117214 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 178762 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 178762 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 212316 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 141313 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 141313 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 178479 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 178479 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 9878 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 9878 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 72547 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 72547 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 72981 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 72981 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 212568 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 187581 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 187581 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 117204 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 117204 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 196217 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 196217 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 178432 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 178432 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 161253 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 161253 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 95929 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 95929 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 196167 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 196167 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 213304 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 79493 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 79493 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 117212 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 117212 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 166072 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 166072 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 60911 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 60911 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 79902 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 79902 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 110643 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 110643 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 78354 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 78354 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 79703 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 79703 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 155376 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 155376 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 132716 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 132716 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 78055 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 78055 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 79811 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 79811 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 133514 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 133514 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 168779 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 168779 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 72368 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 72368 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 60880 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 60880 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 60909 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 60909 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 77761 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 77761 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 171809 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 171809 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 60879 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 60879 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 96657 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 96657 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 97806 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 97806 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 178492 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 178492 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 38021 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 38021 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 73999 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 73999 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 60882 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 60882 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 196427 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 196427 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 166258 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 166258 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 195106 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 195106 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 178761 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 178761 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 195372 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 195372 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 165947 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 165947 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 195428 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 195428 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 96189 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 96189 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 60889 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 60889 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 178434 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 178434 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 77465 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 77465 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 77971 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 77971 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 78084 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 78084 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 73487 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 73487 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 79698 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 79698 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 136027 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 136027 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 96187 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 96187 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 195222 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 195222 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 37971 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 37971 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 38171 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 38171 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 178713 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 178713 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 72344 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 72344 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 77344 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 77344 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 141326 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 141326 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 141326 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 141326 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 141326 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 141326 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 138338 5 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 138338 5 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 117203 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 117203 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 178450 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 178450 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 187190 12 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 187190 12 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 138342 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 138342 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 138639 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 138639 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 139318 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 139318 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 195174 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 195174 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 95839 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 95839 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 60884 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 60884 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 74380 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 74380 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 178631 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 178631 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 60908 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 60908 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 187582 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 187582 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 72054 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 72054 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 189462 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 189462 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 189151 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 189151 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 155575 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 155575 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 196500 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 196500 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 135150 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 135150 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 78680 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 78680 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 60891 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 60891 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 136068 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 136068 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 187506 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 187506 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 193342 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 193342 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 73161 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 73161 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 60906 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 60906 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 72113 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 72113 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 178541 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 178541 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 110611 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 110611 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 60890 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 60890 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 60888 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 60888 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 155672 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 155672 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 60913 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 60913 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 117208 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 117208 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 187474 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 187474 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 74324 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 74324 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 196057 2 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 196057 2 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 178688 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 178688 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 115105 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 115105 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 115105 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 195612 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 195612 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 210670 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 117213 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 117213 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 72185 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 72185 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 117215 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 117215 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 60887 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 60887 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 60886 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 60886 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 72211 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 72211 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 38513 6 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 38513 6 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 161217 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 161217 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 72427 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 72427 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 73632 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 73632 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 60904 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 60904 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 60883 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 60883 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 195437 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 195437 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 73937 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 73937 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 212539 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 72111 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 72111 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 195247 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 195247 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 178709 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 178709 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 196038 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 196038 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 178712 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 178712 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 178685 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 178685 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 156974 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 156974 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 156974 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 156974 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 178442 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 178442 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 195741 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 195741 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 140252 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 140252 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 141304 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 141304 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 95765 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 95765 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 169656 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 169656 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 77908 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 77908 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 195754 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 195754 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 139243 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 139243 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 10090 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 10090 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 60896 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 60896 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 117205 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 117205 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 115105 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 115105 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 115105 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 179800 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 179800 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 181111 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 181111 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 179800 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 179800 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 212795 17 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 181111 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 181111 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 212607 18 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 212607 18 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 212795 17 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 212607 18 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 212607 18 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 169381 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 169381 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 213181 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 210609 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 161018 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 161018 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 3899 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 3899 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 3899 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 2709 9 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 2709 9 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 2709 9 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 2709 9 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 96472 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 96472 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 77573 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 77573 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 212254 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 210556 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 210656 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 213115 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 212251 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 210151 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 213751 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 112662 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 112662 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 112662 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 77578 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 77578 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 112676 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 112676 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 112676 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 57517 0 None 40 3 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 57517 0 None 40 3 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 212685 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 120457 0 None 8 3 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 120457 0 None 8 3 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 2457 29 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 2457 29 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 2457 29 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 78296 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 78296 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 78296 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 83566 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 83566 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 77576 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 77576 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 112624 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 112624 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 112624 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 110093 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 110093 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 112588 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 112588 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 112588 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 112668 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 112668 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 112668 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 112674 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 112674 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 112674 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 210582 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 208494 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 183898 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 183898 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 120534 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 120534 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 120534 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 120534 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 83569 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 83569 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 2392 37 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 2392 37 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 2392 37 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 2392 37 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 77351 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 77351 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 77351 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 77351 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 112590 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 112590 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 112590 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 77358 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 77358 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 77358 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 112596 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 112596 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 112596 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 77572 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 77572 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 77574 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 77574 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 159442 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 159442 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 213131 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 142387 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 142387 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 77575 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 77575 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 77560 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 77560 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 77560 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 77560 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 112675 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 112675 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 112675 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 112589 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 112589 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 112589 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 212832 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 183899 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 183899 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 57277 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 57277 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 77564 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 77564 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 78306 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 78306 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 78306 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 112608 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 112608 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 112608 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 77564 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 77564 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 112659 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 112659 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 112659 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 210754 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 183772 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 183772 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 112606 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 112606 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 112606 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 120539 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 120539 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 120539 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 77579 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 77579 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 191185 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 191185 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 7578 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 7578 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 174046 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 174046 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 183920 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 183920 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 77561 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 77561 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 77561 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 77561 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 1039 26 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 1039 26 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 1039 26 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 213080 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 188346 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 188346 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 169198 1 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 169198 1 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 78305 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 78305 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 78305 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 3360 0 None 1 7 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 3360 0 None 1 7 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 3360 0 None 1 7 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 208493 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 3521 31 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 3521 31 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 3521 31 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 147159 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 147159 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 174194 3 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 174194 3 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 183771 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 183771 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 120534 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 120534 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 120534 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 120534 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 139158 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 139158 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 212728 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 205135 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 205135 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 3503 15 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 3503 15 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 3503 15 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 77565 26 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 77565 26 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 208492 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 2832 18 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 2832 18 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 2832 18 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 112618 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 112618 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 112618 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 172237 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 172237 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 161253 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 161253 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 161253 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 161253 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 77577 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 77577 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 210501 8 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 87338 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 87338 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 179333 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 179333 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 189689 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 189689 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 171104 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 171104 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 120533 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 120533 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 120533 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 2094 23 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 2094 23 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 2094 23 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 3360 0 None -1 7 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 3360 0 None -1 7 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 3360 0 None -1 7 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 212929 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 107016 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 107016 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 77570 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 77570 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 77570 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 185743 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 185743 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 213169 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 194657 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 194657 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 120502 0 None -2 3 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 120502 0 None -2 3 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 87722 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 87722 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 87901 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 87901 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 154376 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 154376 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 154725 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 154725 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 169326 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 169326 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 179200 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 179200 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 179282 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 179282 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 179462 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 179462 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 180468 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 180468 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 189792 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 189792 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 145494 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 145494 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 120528 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 120528 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 120528 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 120531 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 120531 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 120531 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 96173 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 96173 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 99142 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 99142 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 67726 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 67726 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 107099 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 107099 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 183941 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 183941 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 212252 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 153592 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 153592 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 214263 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 78608 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 78608 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 120541 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 120541 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 120541 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 2829 28 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 85676 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 85676 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 86844 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 86844 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 179091 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 179091 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 189566 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 189566 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 5836 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 5836 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 213359 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 2832 18 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 2832 18 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 2832 18 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 191274 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 191274 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 99142 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 99142 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 112615 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 112615 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 152046 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 152046 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 78605 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 78605 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 99637 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 99637 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 142064 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 142064 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 142064 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 142064 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 86987 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 86987 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 87339 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 87339 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 179093 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 179093 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 180816 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 180816 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 189631 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 189631 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 174576 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 174576 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 6011 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 6011 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 146411 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 146411 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 62621 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 62621 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 57276 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 57276 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 78611 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 78611 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 2832 18 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 2832 18 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 2832 18 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 212404 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 212549 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 179281 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 179281 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 189999 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 189999 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 91181 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 91181 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 170845 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 170845 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 147296 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 147296 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 210752 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 96129 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 96129 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 212979 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 86833 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 86833 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 180276 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 180276 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 189542 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 189542 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 189623 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 189623 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 91103 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 91103 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 2832 18 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 2832 18 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 2832 18 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 120605 0 None -3 3 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 120605 0 None -3 3 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 57282 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 57282 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 76636 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 76636 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 212606 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 103373 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 103373 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 85681 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 85681 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 179277 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 179277 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 179334 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 179334 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 91199 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 91199 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 145494 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 145494 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 145494 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 145494 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 148631 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 148631 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 120532 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 120532 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 120532 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 210630 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 213664 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 87519 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 87519 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 186303 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 186303 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 144959 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 144959 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 171631 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 171631 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 120536 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 120536 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 120536 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 120545 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 120545 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 120545 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 125775 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 125775 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 3337 21 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 3337 21 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 3337 21 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 99637 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 99637 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 95884 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 95884 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 78608 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 78608 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 105420 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 105420 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 113964 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 113964 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 147960 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 147960 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 91102 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 91102 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 91102 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 91102 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 7592 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 7592 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 4377 16 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 4377 16 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 4377 16 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 4377 16 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 99079 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 99079 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 179355 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 179355 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 189547 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 189547 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 98243 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 98243 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 148446 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 148446 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 4377 16 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 4377 16 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 4377 16 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 4377 16 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 96064 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 96064 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 150111 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 150111 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 57278 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 57278 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 173931 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 173931 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 179457 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 179457 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 166573 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 166573 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 120436 0 None -1 3 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 120436 0 None -1 3 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 95941 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 95941 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 143383 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 143383 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 102895 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 102895 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 205049 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 205049 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 153269 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 153269 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 87494 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 87494 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 179953 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 179953 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 173692 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 173692 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 77567 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 77567 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 78609 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 78609 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 78610 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 78610 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 96369 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 96369 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 189300 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 189300 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 179602 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 179602 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 183921 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 183921 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 7526 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 7526 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 96129 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 96129 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 138924 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 138924 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 214421 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 30866 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 30866 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 31776 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 31776 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 168271 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 168271 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 87902 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 87902 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 189147 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 189147 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 212572 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 77570 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 77570 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 77570 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 161008 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 161008 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 86739 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 86739 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 178412 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 178412 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 120526 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 120526 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 120526 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 120429 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 120429 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 210640 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 67726 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 67726 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 96174 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 96174 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 212795 17 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 151269 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 151269 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 103366 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 103366 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 79914 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 79914 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 115302 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 115302 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 189356 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 189356 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 178638 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 178638 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 189387 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 189387 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 103303 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 103303 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 103309 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 103309 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 103312 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 103312 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 103313 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 103313 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 103316 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 103316 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 205099 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 205099 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 205137 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 205137 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 145537 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 145537 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 120544 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 120544 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 120544 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 96947 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 96947 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 138992 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 138992 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 83565 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 83565 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 175144 3 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 175144 3 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 171268 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 171268 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 122598 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 122598 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 91746 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 91746 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 147365 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 147365 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 212607 18 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 212607 18 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 212640 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 97753 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 97753 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 178764 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 178764 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 102854 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 102854 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 143670 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 143670 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 141976 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 141976 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 76626 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 76626 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 145494 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 145494 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 152291 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 152291 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 109658 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 109658 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 152900 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 152900 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 208749 19 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 97674 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 97674 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 115285 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 115285 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 147960 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 147960 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 163327 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 163327 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 110924 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 110924 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 6021 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 6021 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 96804 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 96804 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 148594 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 148594 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 5455 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 5455 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 6843 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 6843 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 62619 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 62619 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 147296 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 147296 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 150596 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 150596 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 64840 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 64840 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 178456 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 178456 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 3872 40 None -794 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 3872 40 None -794 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 3872 40 None -794 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 3872 40 None -794 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 148327 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 148327 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 101691 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 101691 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 65580 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 65580 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 122598 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 122598 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 142091 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 142091 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 86824 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 86824 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 115300 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 115300 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 115314 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 115314 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 179106 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 179106 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 186285 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 186285 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 178490 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 178490 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 178524 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 178524 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 74981 48 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 74981 48 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 176190 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 176190 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 6152 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 6152 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 112558 11 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 112558 11 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 112558 11 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 173332 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 173332 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 110981 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 110981 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 80085 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 80085 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 80085 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 90434 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 90434 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 91742 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 91742 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 128151 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 128151 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 76631 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 76631 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 4327 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 4327 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 96128 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 96128 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 31645 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 31645 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 87720 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 87720 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 120527 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 120527 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 120527 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 108502 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 108502 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 96737 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 96737 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 5841 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 5841 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 168287 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 168287 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 5480 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 5480 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 132013 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 132013 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 9131 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 9131 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 78262 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 78262 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 88198 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 88198 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 62617 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 62617 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 144499 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 144499 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 109638 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 109638 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 115275 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 115275 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 135155 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 135155 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 145418 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 145418 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 149415 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 149415 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 169402 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 169402 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 115310 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 115310 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 91689 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 91689 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 8597 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 8597 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 8597 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 8597 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 165867 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 165867 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 97553 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 97553 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 85669 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 85669 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 86738 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 86738 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 115315 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 115315 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 179111 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 179111 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 103314 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 103314 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 189158 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 189158 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 110980 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 110980 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 90315 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 90315 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 147608 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 147608 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 170641 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 170641 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 124309 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 124309 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 120445 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 120445 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 188189 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 188189 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 179121 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 179121 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 90436 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 90436 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 77566 32 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 77566 32 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 113912 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 113912 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 32332 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 32332 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 103301 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 103301 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 99321 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 99321 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 99609 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 99609 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 64984 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 64984 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 85680 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 85680 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 69779 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 69779 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 212929 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 143383 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 143383 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 101167 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 101167 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 65433 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 65433 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 9382 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 9382 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 121280 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 121280 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 87795 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 87795 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 76623 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 76623 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 88028 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 88028 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 172139 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 172139 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 85658 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 85658 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 85658 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 85658 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 85658 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 85658 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 178411 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 178411 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 103323 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 103323 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 128171 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 128171 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 34624 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 34624 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 76633 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 76633 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 145418 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 145418 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 2576 20 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 2576 20 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 2576 20 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 2576 20 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 2576 20 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 97669 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 97669 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 112839 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 112839 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 150099 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 150099 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 85678 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 85678 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 91690 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 91690 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 65675 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 65675 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 85657 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 85657 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 5221 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 5221 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 111588 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 111588 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 168235 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 168235 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 95977 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 95977 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 86698 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 86698 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 172982 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 172982 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 142458 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 142458 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 107300 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 107300 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 64445 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 64445 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 103354 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 103354 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 85938 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 85938 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 86736 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 86736 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 189399 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 189399 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 91191 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 91191 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 169353 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 169353 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 91743 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 91743 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 178658 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 178658 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 124310 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 124310 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 87492 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 87492 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 121383 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 121383 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 156928 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 156928 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 147238 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 147238 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 66975 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 66975 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 213333 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 153814 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 153814 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 96761 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 96761 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 86988 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 86988 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 147886 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 147886 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 115289 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 115289 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 103294 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 103294 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 103304 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 103304 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 7417 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 7417 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 91768 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 91768 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 148651 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 148651 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 90430 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 90430 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 99775 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 99775 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 4299 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 4299 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 172271 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 172271 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 108524 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 108524 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 213134 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 104861 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 104861 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 189766 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 189766 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 173037 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 173037 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 112840 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 112840 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 175524 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 175524 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 7713 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 7713 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 128164 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 128164 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 110665 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 110665 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 90599 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 90599 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 154611 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 154611 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 128160 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 128160 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 178632 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 178632 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 62620 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 62620 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 65679 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 65679 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 90595 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 90595 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 99071 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 99071 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 153434 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 153434 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 87493 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 87493 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 178525 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 178525 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 103305 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 103305 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 65676 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 65676 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 5867 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 5867 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 77857 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 77857 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 120538 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 120538 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 120538 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 145104 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 145104 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 85710 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 85710 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 144499 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 144499 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 138917 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 138917 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 129014 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 129014 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 86653 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 86653 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 32850 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 32850 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 32850 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 151988 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 151988 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 149568 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 149568 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 115281 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 115281 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 115303 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 115303 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 179105 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 179105 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 103318 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 103318 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 189362 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 189362 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 91268 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 91268 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 83570 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 83570 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 156619 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 156619 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 212780 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 151188 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 151188 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 174365 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 174365 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 209980 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 115294 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 115294 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 129013 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 129013 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 148268 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 148268 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 154165 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 154165 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 128167 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 128167 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 129017 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 129017 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 210530 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 125774 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 125774 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 152612 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 152612 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 103347 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 103347 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 79720 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 79720 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 86573 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 86573 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 179111 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 179111 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 6020 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 6020 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 66943 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 66943 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 138997 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 138997 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 179351 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 179351 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 65673 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 65673 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 90440 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 90440 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 139041 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 139041 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 151207 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 151207 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 97704 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 97704 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 87486 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 87486 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 79082 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 79082 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 5176 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 5176 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 171631 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 171631 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 97428 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 97428 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 156466 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 156466 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 7640 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 7640 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 110935 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 110935 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 66181 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 66181 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 123615 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 123615 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 110984 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 110984 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 85662 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 85662 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 194952 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 194952 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 147695 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 147695 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 85929 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 85929 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 189181 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 189181 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 103308 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 103308 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 91203 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 91203 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 189752 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 189752 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 193397 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 193397 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 141572 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 141572 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 141572 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 213131 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 149178 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 149178 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 152291 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 152291 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 167903 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 167903 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 123044 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 123044 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 128168 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 128168 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 110934 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 110934 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 172438 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 172438 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 178456 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 178456 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 85928 78 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 85928 78 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 213030 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 195233 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 195233 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 196161 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 196161 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 79903 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 79903 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 85690 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 85690 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 142064 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 142064 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 142064 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 142064 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 86696 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 86696 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 178578 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 178578 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 91747 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 91747 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 170622 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 170622 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 90625 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 90625 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 91201 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 91201 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 145690 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 145690 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 145710 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 145710 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 166372 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 166372 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 113963 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 113963 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 171809 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 171809 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 57529 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 57529 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 77568 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 77568 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 77568 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 78604 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 78604 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 98243 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 98243 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 179777 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 179777 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 180279 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 180279 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 191837 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 191837 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 110975 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 110975 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 78606 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 78606 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 189714 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 189714 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 169809 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 169809 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 78607 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 78607 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 118977 1 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 118977 1 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 212527 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 163151 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 163151 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 86740 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 86740 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 138974 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 138974 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 175333 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 175333 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 176382 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 176382 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 176382 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 116652 1 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 116652 1 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 2094 23 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 2094 23 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 2094 23 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 189253 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 189253 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 91260 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 91260 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 179358 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 179358 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 91260 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 91260 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 172947 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 172947 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 6006 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 6006 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 95832 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 95832 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 91762 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 91762 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 138991 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 138991 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 125770 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 125770 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 152663 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 152663 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 98607 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 98607 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 99214 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 99214 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 183806 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 183806 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 5868 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 5868 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 212972 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 96402 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 96402 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 190745 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 190745 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 33970 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 33970 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 148407 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 148407 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 66112 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 66112 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 149007 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 149007 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 178604 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 178604 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 6017 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 6017 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 175237 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 175237 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 99562 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 99562 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 98586 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 98586 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 172371 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 172371 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 6153 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 6153 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 110978 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 110978 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 213114 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 147238 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 147238 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 65095 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 65095 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 115292 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 115292 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 115304 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 115304 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 115305 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 115305 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 186545 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 186545 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 178553 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 178553 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 103291 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 103291 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 91724 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 91724 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 91769 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 91769 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 113963 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 113963 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 35236 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 35236 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 90439 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 90439 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 163142 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 163142 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 176610 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 176610 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 176610 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 108718 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 108718 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 108718 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 108718 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 108718 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 108718 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 125771 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 125771 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 189609 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 189609 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 113863 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 113863 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 151332 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 151332 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 146954 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 146954 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 142387 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 142387 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 97867 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 97867 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 143231 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 143231 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 186284 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 186284 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 6325 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 6325 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 159889 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 159889 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 149084 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 149084 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 115306 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 115306 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 90431 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 90431 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 120950 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 120950 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 136975 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 136975 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 164631 23 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 164631 23 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 6255 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 6255 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 176040 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 176040 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 173847 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 173847 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 86652 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 86652 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 63871 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 63871 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 97585 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 97585 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 77570 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 77570 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 77570 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 78647 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 78647 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 103359 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 103359 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 189327 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 189327 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 103297 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 103297 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 65674 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 65674 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 5936 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 5936 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 146866 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 146866 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 128152 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 128152 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 110570 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 110570 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 85670 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 85670 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 91677 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 91677 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 66232 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 66232 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 166257 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 166257 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 5840 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 5840 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 6189 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 6189 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 128156 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 128156 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 66277 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 66277 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 103365 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 103365 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 157379 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 157379 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 142064 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 142064 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 142064 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 142064 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 150973 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 150973 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 153237 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 153237 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 91547 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 91547 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 91547 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 91547 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 90598 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 90598 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 173125 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 173125 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 174529 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 174529 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 148409 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 148409 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 66133 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 66133 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 7435 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 7435 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 179980 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 179980 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 153814 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 153814 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 107238 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 107238 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 65677 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 65677 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 65541 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 65541 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 99262 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 99262 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 103358 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 103358 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 147100 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 147100 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 115284 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 115284 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 179105 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 179105 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 171707 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 171707 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 121375 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 121375 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 115295 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 115295 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 71809 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 71809 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 91098 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 91098 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 123287 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 123287 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 103362 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 103362 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 189317 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 189317 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 96612 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 96612 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 213051 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 153841 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 153841 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 91101 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 91101 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 212843 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 213311 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 213735 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 208098 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 208098 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 7486 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 7486 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 108591 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 108591 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 7497 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 7497 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 7498 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 7498 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 108504 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 108504 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 9166 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 9166 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 161280 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 161280 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 144252 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 144252 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 189742 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 189742 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 121378 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 121378 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 76627 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 76627 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 76628 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 76628 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 90433 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 90433 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 1301 45 None -28 9 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 1301 45 None -28 9 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 1301 45 None -28 9 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 1301 45 None -28 9 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 97641 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 97641 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 127267 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 127267 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 79693 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 79693 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 79693 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 106738 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 106738 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 168746 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 168746 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 115287 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 115287 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 115298 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 115298 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 172201 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 172201 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 140341 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 140341 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 78418 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 78418 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 103360 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 103360 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 2478 45 None -186 6 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 2478 45 None -186 6 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 2478 45 None -186 6 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 2478 45 None -186 6 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 62576 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 62576 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 6005 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 6005 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 194970 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 194970 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 66125 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 66125 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 158709 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 158709 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 179141 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 179141 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 63851 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 63851 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 178462 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 178462 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 76630 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 76630 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 103370 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 103370 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 115283 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 115283 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 103295 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 103295 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 6016 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 6016 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 90314 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 90314 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 91387 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 91387 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 4418 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 4418 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 171274 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 171274 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 95862 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 95862 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 139116 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 139116 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 79745 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 79745 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 120537 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 120537 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 120537 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 128162 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 128162 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 146793 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 146793 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 146411 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 146411 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 85656 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 85656 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 5842 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 5842 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 146113 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 146113 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 189181 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 189181 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 96409 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 96409 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 196111 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 196111 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 85698 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 85698 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 143964 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 143964 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 178485 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 178485 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 189182 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 189182 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 189420 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 189420 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 103290 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 103290 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 103317 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 103317 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 103321 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 103321 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 90597 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 90597 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 90599 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 90599 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 90859 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 90859 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 91868 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 91868 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 145493 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 145493 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 76632 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 76632 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 97972 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 97972 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 139009 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 139009 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 110977 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 110977 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 177665 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 177665 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 154985 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 154985 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 98623 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 98623 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 168615 0 None 2 3 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 168615 0 None 2 3 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 166677 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 166677 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 178516 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 178516 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 110976 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 110976 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 189221 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 189221 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 176771 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 176771 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 147274 1 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 147274 1 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 7487 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 7487 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 95853 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 95853 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 139054 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 139054 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 188816 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 188816 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 189148 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 189148 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 213442 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 179161 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 179161 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 190055 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 190055 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 120543 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 120543 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 120543 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 66112 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 66112 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 159527 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 159527 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 76635 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 76635 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 188330 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 188330 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 96401 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 96401 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 66950 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 66950 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 163298 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 163298 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 90428 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 90428 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 213503 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 103496 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 103496 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 163340 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 163340 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 7698 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 7698 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 186547 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 186547 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 133556 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 133556 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 8916 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 8916 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 107238 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 107238 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 115309 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 115309 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 178554 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 178554 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 103298 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 103298 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 189081 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 189081 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 6010 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 6010 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 76629 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 76629 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 176052 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 176052 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 140477 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 140477 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 148639 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 148639 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 188830 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 188830 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 212653 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 212986 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 213399 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 129643 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 129643 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 128157 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 128157 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 58692 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 58692 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 5293 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 5293 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 85937 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 85937 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 136977 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 136977 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 152046 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 152046 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 66643 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 66643 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 115282 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 115282 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 106740 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 106740 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 7849 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 7849 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 121487 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 121487 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 103371 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 103371 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 86986 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 86986 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 115288 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 115288 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 180465 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 180465 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 121371 0 None -676 3 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 121371 0 None -676 3 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 152841 0 None -676 3 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 152841 0 None -676 3 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 121371 0 None -676 3 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 121371 0 None -676 3 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 151813 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 151813 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 110938 0 None -85 3 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 110938 0 None -85 3 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 110938 0 None -85 3 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 110938 0 None -85 3 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 66203 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 66203 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 110471 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 110471 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 120864 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 120864 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 85664 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 85664 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 115280 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 115280 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 7401 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 7401 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 128155 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 128155 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 78519 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 78519 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 143967 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 143967 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 66246 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 66246 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 64834 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 64834 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 103319 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 103319 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 91739 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 91739 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 149441 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 149441 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 150099 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 150099 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 9261 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 9261 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 30900 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 30900 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 110418 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 110418 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 64638 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 64638 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 168932 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 168932 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 31709 1 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 31709 1 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 66862 1 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 66862 1 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 153247 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 153247 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 90625 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 90625 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 189387 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 189387 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 153550 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 153550 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 140485 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 140485 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 64984 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 64984 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 178413 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 178413 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 99926 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 99926 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 64856 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 64856 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 115273 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 115273 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 115312 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 115312 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 212253 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 167835 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 167835 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 97921 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 97921 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 142882 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 142882 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 110927 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 110927 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 210572 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 128161 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 128161 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 166372 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 166372 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 139328 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 139328 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 85677 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 85677 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 143228 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 143228 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 115286 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 115286 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 189283 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 189283 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 103292 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 103292 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 90348 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 90348 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 90594 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 90594 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 90599 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 90599 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 90625 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 90625 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 145414 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 145414 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 166372 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 166372 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 128169 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 128169 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 179250 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 179250 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 90625 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 90625 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 168728 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 168728 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 96176 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 96176 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 57281 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 57281 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 57283 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 57283 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 57284 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 57284 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 179131 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 179131 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 189419 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 189419 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 120540 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 120540 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 120540 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 179141 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 179141 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 189218 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 189218 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 120535 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 120535 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 120535 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 77562 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 77562 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 57275 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 57275 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 77562 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 77562 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 87518 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 87518 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 175839 5 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 175839 5 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 144960 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 144960 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 58712 0 None 1 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 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 58712 0 None 1 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 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 107874 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 107874 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 97715 1 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 97715 1 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 7485 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 7485 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 57457 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 57457 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 156373 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 156373 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 158282 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 158282 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 147181 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 147181 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 178607 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 178607 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 189156 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 189156 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 66157 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 66157 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 90441 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 90441 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 139849 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 139849 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 103302 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 103302 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 146268 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 146268 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 77568 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 77568 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 77568 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 85912 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 85912 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 70289 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 70289 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 5977 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 5977 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 86574 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 86574 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 123975 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 123975 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 120245 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 120245 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 125862 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 125862 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 95799 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 95799 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 99150 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 99150 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 135188 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 135188 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 97271 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 97271 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 132464 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 132464 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 97932 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 97932 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 85692 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 85692 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 103315 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 103315 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 140343 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 140343 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 111355 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 111355 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 154165 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 154165 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 125776 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 125776 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 110925 0 None -295 5 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 110925 0 None -295 5 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 110925 0 None -295 5 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 110925 0 None -295 5 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 110925 0 None -295 5 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 110925 0 None -295 5 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 110925 0 None -295 5 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 110925 0 None -295 5 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 171038 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 171038 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 87716 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 87716 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 151813 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 151813 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 163172 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 163172 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 98366 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 98366 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 142063 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 142063 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 127369 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 127369 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 96975 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 96975 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 5935 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 5935 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 121381 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 121381 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 169821 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 169821 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 67026 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 67026 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 106735 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 106735 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 128154 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 128154 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 5866 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 5866 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 88173 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 88173 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 88029 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 88029 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 33075 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 33075 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 33075 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 168948 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 168948 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 66149 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 66149 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 30725 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 30725 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 96698 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 96698 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 110939 0 None -29512 3 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 110939 0 None -29512 3 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 143615 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 143615 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 103361 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 103361 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 103306 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 103306 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 140353 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 140353 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 166372 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 166372 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 179226 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 179226 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 121379 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 121379 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 6188 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 6188 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 5481 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 5481 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 87337 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 87337 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 143563 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 143563 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 180614 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 180614 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 62618 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 62618 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 5479 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 5479 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 7703 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 7703 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 179014 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 179014 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 145783 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 145783 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 148327 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 148327 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 172844 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 172844 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 103346 9 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 103346 9 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 103349 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 103349 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 85672 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 85672 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 144703 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 144703 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 115276 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 115276 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 189120 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 189120 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 5938 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 5938 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 90626 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 90626 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 91202 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 91202 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 145155 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 145155 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 65416 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 65416 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 204841 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 204841 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 77571 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 77571 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 189299 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 189299 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 7516 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 7516 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 90437 1 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 90437 1 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 189438 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 189438 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 77357 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 77357 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 83568 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 83568 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 143192 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 143192 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 179010 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 179010 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 113962 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 113962 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 120529 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 120529 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 120529 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 87903 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 87903 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 7527 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 7527 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 80265 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 80265 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 80265 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 139129 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 139129 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 76622 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 76622 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 99511 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 99511 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 128173 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 128173 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 77563 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 77563 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 77563 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 77563 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 107195 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 107195 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 138978 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 138978 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 191705 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 191705 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 125771 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 125771 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 172407 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 172407 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 171466 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 171466 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 95892 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 95892 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 96031 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 96031 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 148955 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 148955 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 115293 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 115293 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 115311 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 115311 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 116509 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 116509 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 1651 49 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 1651 49 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 1651 49 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 1651 49 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 1651 49 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 210621 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 66947 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 66947 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 123745 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 123745 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 153816 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 153816 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 79078 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 79078 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 97969 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 97969 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 86737 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 86737 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 186697 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 186697 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 128172 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 128172 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 65718 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 65718 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 77978 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 77978 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 77978 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 63429 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 63429 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 138356 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 138356 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 120380 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 120380 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 128163 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 128163 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 150063 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 150063 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 85668 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 85668 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 189727 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 189727 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 149363 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 149363 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 153247 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 153247 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 101709 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 101709 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 85699 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 85699 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 126363 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 126363 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 97673 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 97673 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 148660 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 148660 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 115274 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 115274 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 139039 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 139039 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 103320 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 103320 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 180617 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 180617 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 121376 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 121376 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 121377 0 None -794 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 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 121377 0 None -794 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 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 128174 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 128174 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 168438 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 168438 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 146113 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 146113 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 77627 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 77627 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 189561 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 189561 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 5195 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 5195 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 121382 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 121382 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 7700 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 7700 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 115290 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 115290 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 191167 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 191167 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 62614 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 62614 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 62615 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 62615 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 128166 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 128166 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 154951 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 154951 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 85708 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 85708 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 66842 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 66842 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 148184 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 148184 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 103355 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 103355 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 85691 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 85691 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 115277 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 115277 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 115301 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 115301 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 189430 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 189430 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 178577 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 178577 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 178763 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 178763 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 103296 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 103296 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 103311 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 103311 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 107265 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 107265 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 154954 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 154954 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 107265 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 107265 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 66112 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 66112 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 97403 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 97403 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 91100 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 91100 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 33195 6 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 33195 6 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 33195 6 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 5462 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 5462 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 31018 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 31018 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 90435 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 90435 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 57279 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 57279 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 158952 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 158952 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 213116 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 179283 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 179283 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 99470 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 99470 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 91779 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 91779 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 91779 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 91779 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 65574 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 65574 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 62616 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 62616 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 171678 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 171678 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 59307 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 59307 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 129015 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 129015 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 66278 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 66278 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 91180 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 91180 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 128159 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 128159 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 85910 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 85910 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 139923 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 139923 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 88197 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 88197 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 115297 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 115297 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 7515 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 7515 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 121380 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 121380 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 145669 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 145669 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 65562 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 65562 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 133415 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 133415 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 128158 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 128158 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 147181 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 147181 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 64537 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 64537 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 128150 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 128150 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 213142 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 96999 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 96999 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 149112 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 149112 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 110473 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 110473 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 174276 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 174276 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 172649 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 172649 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 128149 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 128149 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 9293 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 9293 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 179201 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 179201 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 166330 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 166330 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 65678 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 65678 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 115296 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 115296 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 87721 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 87721 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 168799 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 168799 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 178605 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 178605 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 115308 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 115308 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 172844 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 172844 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 129016 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 129016 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 5183 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 5183 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 109152 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 109152 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 103353 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 103353 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 70593 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 70593 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 9067 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 9067 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 97442 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 97442 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 31195 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 31195 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 103368 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 103368 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 115278 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 115278 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 115291 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 115291 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 189441 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 189441 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 103293 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 103293 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 103310 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 103310 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 141644 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 141644 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 141644 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 6009 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 6009 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 59130 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 59130 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 97379 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 97379 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 99533 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 99533 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 178421 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 178421 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 77568 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 77568 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 77568 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 144472 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 144472 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 189280 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 189280 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 120523 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 120523 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 120523 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 125023 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 125023 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 4594 3 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 4594 3 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 4594 3 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 4594 3 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 178515 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 178515 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 90429 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 90429 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 5937 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 5937 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 95893 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 95893 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 115307 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 115307 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 195281 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 195281 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 208383 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 208383 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 79913 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 79913 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 124626 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 124626 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 110186 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 110186 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 106737 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 106737 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 85709 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 85709 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 103299 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 103299 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 145104 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 145104 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 5154 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 5154 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 148378 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 148378 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 115313 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 115313 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 97640 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 97640 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 5392 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 5392 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 103300 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 103300 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 110938 0 None -85 3 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 110938 0 None -85 3 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 140677 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 140677 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 151115 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 151115 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 110982 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 110982 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 32959 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 32959 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 32959 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 64428 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 64428 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 189141 1 None -812 6 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 143563 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 143563 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 5164 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 5164 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 125490 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 125490 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 120542 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 120542 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 120542 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 100591 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 100591 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 5223 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 5223 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 103322 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 103322 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 121369 0 None -1995 3 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 121369 0 None -1995 3 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 96939 0 None -1995 3 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 96939 0 None -1995 3 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 121369 0 None -1995 3 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 121369 0 None -1995 3 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 121476 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 121476 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 189360 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 189360 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 177666 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 177666 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 71868 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 71868 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 2141 29 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 2141 29 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 2141 29 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 2141 29 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 2141 29 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 2141 29 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 178489 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 178489 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 65238 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 65238 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 91748 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 91748 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 65671 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 65671 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 99502 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 99502 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 139100 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 139100 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 110979 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 110979 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 174778 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 174778 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 90438 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 90438 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 97922 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 97922 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 128153 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 128153 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 121373 0 None -1995 3 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 121373 0 None -1995 3 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 144484 0 None -1995 3 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 144484 0 None -1995 3 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 121373 0 None -1995 3 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 121373 0 None -1995 3 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 57280 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 57280 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 138919 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 138919 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 139527 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 139527 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 95934 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 95934 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 120530 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 120530 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 120530 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 66075 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 66075 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 85663 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 85663 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 115279 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 115279 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 165030 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 165030 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 138396 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 138396 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 121374 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 121374 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 80196 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 80196 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 80196 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 99477 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 99477 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 91691 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 91691 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 110616 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 110616 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 179202 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 179202 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 123658 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 123658 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 62622 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 62622 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 65909 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 65909 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 168790 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 168790 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 168790 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 179455 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 179455 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 87485 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 87485 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 34911 1 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 34911 1 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 144785 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 144785 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 9313 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 9313 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 9313 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 9313 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 78984 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 78984 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 119203 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 119203 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 112841 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 112841 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 99300 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 99300 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 189687 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 189687 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 128165 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 128165 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 213168 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 144785 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 144785 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 103348 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 103348 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 103367 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 103367 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 85682 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 85682 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 161724 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 161724 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 103307 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 103307 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 166838 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 166838 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 168976 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 168976 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 125773 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 125773 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 83567 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 83567 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 77569 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 77569 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 120524 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 120524 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 120524 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 172113 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 172113 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 95778 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 95778 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 154726 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 154726 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 169513 3 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 169513 3 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 76634 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 76634 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 90432 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 90432 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 153269 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 153269 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 97918 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 97918 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 64814 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 64814 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 189365 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 189365 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 95883 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 95883 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 87319 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 87319 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 97982 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 97982 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 149446 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 149446 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 9130 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 9130 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 108667 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 108667 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 79925 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 79925 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 149112 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 149112 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 153816 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 153816 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 156166 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 156166 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 67192 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 67192 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 135990 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 135990 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 121368 0 None -1230 3 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 121368 0 None -1230 3 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 207634 0 None -1230 3 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 207634 0 None -1230 3 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 121368 0 None -1230 3 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 121368 0 None -1230 3 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 141510 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 141510 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 115299 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 115299 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 153015 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 153015 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 151140 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 151140 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 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
16131448 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1681 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1688 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
44361543 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
56947112 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
CHEMBL396460 2829 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1685 3898 0 None - 1 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15509719
23383556 179333 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 179333 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 189689 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 189689 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 179200 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 179200 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 179282 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 179282 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 179462 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 179462 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 180468 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 180468 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 189792 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 189792 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 179091 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 179091 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 189566 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 189566 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 179093 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 179093 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 180816 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 180816 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 189631 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 189631 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 179281 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 179281 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 189999 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 189999 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 180276 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 180276 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 189542 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 189542 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 189623 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 189623 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 179277 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 179277 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 179334 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 179334 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 91102 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 91102 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 179355 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 179355 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 189547 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 189547 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 179457 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 179457 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 179953 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 179953 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 179602 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 179602 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 189147 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 189147 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 216279 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 217445 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 217447 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 217448 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 217449 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 188189 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 188189 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 179121 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 179121 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 189766 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 189766 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 179351 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 179351 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 189752 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 189752 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 179777 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 179777 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 180279 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 180279 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 189714 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 189714 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 175333 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 175333 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 91260 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 91260 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 179358 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 179358 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 190745 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 190745 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 175237 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 175237 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 189609 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 189609 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 91547 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 91547 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 179980 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 179980 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 189742 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 189742 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 177665 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 177665 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 176771 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 176771 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 189148 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 189148 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 190055 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 190055 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 188330 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 188330 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 189081 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 189081 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 180465 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 180465 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 179250 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 179250 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 217446 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 189218 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 189218 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 179226 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 179226 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 180614 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 180614 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 189120 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 189120 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 179010 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 179010 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 1651 49 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 1651 49 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 1651 49 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 1651 49 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 1651 49 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 189727 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 189727 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 180617 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 180617 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 189561 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 189561 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 1651 49 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 1651 49 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 1651 49 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 1651 49 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 1651 49 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 179283 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 179283 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 91779 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 91779 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 179201 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 179201 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 215977 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 2576 20 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 2576 20 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 2576 20 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 2576 20 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 2576 20 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 177666 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 177666 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 174778 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 174778 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 179202 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 179202 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 179455 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 179455 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 189687 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 189687 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 2457 29 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 2457 29 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 2457 29 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 3641 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 3641 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 3641 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 3528 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 3528 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 507 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 507 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 507 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 3521 31 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 3521 31 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 3521 31 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 874 52 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 3521 31 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 3521 31 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 3521 31 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 3521 31 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 3521 31 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 3521 31 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 2392 37 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 2392 37 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 2392 37 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 2392 37 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 2392 37 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 2392 37 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 2392 37 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 2392 37 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 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
16131448 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
16131448 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1681 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1681 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1681 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1688 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1688 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1688 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
44361543 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
44361543 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
44361543 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
56947112 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
56947112 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
56947112 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
CHEMBL396460 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL396460 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL396460 2829 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1694 3897 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
25081457 3897 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1682 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1682 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1682 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1682 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
6324645 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
6324645 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
6324645 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
6324645 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
CHEMBL384755 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL384755 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL384755 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL384755 2832 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
8865 3214 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24903280
1686 3051 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1686 3051 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15743186
50922685 731 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 731 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 2094 23 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 2094 23 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 2094 23 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 268 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1679 268 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 268 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
9963005 268 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 268 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL437723 268 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
132427684 508 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 508 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3503 15 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 3337 21 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 3337 21 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 3337 21 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 3337 21 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 3337 21 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 3337 21 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 269 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1680 269 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
15512229 3360 0 None 1 7 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 3360 0 None 1 7 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 3360 0 None 1 7 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 1039 26 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 1039 26 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 1039 26 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 2700 26 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 2700 26 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 2700 26 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 2700 26 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 2700 26 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 2833 0 None - 1 Human 10.4 pKi None 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1696 3029 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
5311338 3029 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
1692 2141 29 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 2141 29 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 2141 29 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 2855 0 None - 1 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1679 268 24 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 268 24 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 268 24 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1680 269 0 None -2 2 Mouse 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1690 1623 0 None - 1 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
16131448 2829 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2829 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2829 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2829 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2829 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2829 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
16143911 466 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
1689 466 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
CHEMBL505874 466 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863