Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

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weight		 Rot
Bonds		 H don

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 DOI
25208097 183922 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 183922 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 3930 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 3930 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 3930 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 208818 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 208818 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 210632 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 161853 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 161853 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 159840 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 159840 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 97863 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 97863 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 97863 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 212751 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 210524 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 210174 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 210663 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 96501 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 96501 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 213002 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 212572 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 208811 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 213382 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 169405 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 169405 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 2852 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 2852 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 2852 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 208812 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 208812 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2474 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 2474 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 2474 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 161853 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 161853 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 210579 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 183922 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 183922 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 2852 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 2852 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 2852 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 3930 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 3930 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 3930 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 213526 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 208816 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 208816 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 3930 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 3930 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 3930 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 208517 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 159840 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 159840 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 213154 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 2852 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 2852 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 2852 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 214557 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 208818 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 213465 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 169405 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 169405 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 161853 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 161853 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 467 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 467 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 467 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 215593 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 467 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 467 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 467 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2852 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 2852 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 2852 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 159840 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 159840 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 214213 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 183796 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 183796 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 120565 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 120565 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 120565 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 215735 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 215743 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 191209 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 191209 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 212595 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 208516 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 183923 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 183923 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 183944 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 183944 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 188370 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 188370 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 77594 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 77594 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 214299 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 210632 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 213739 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 214244 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 214691 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 215406 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 214185 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 210534 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 90469 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 90469 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 214444 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 178577 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 178577 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 90458 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 90458 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 213910 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 214180 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 215682 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2852 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 2852 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 2852 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 103317 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 103317 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2852 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 2852 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 2852 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 120560 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 120560 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 120560 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 120560 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 65706 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 65706 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 214617 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 213910 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 143253 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 143253 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 189165 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 189165 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 189165 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 169845 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 169845 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 85727 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 85727 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 108551 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 108551 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 208406 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 208406 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 214527 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 215657 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 66142 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 66142 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 3547 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 3547 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 3547 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 57308 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 57308 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 213770 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 213708 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 120483 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 120483 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 212427 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 120558 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 120558 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 120558 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 174218 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 174218 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 77595 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 77595 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 215091 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 111009 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 111009 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 115314 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 115314 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 90468 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 90468 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 115315 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 115315 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 212427 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 183945 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 183945 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 877 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 877 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 877 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 877 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 877 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 215029 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 168771 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 168771 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 56428 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 56428 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 210644 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 14120 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 14120 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 14120 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 178787 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 178787 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 90462 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 90462 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 176406 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 176406 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 176406 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 66142 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 66142 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 56428 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 56428 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 178549 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 178549 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 121395 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 121395 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 103347 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 103347 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 144455 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 144455 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 144455 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 210173 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 210173 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 121399 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 121399 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 189165 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 189165 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 189165 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 215626 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 14179 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 14179 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 14179 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 212427 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 99539 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 99539 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 214747 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 174553 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 174553 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 115304 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 115304 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 213667 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 121684 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 121684 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 121684 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 66187 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 66187 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 178436 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 178436 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 178628 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 178628 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 107222 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 107222 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 210750 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 212501 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 66155 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 66155 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 169537 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 169537 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 121406 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 121406 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 66163 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 66163 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 189277 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 189277 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 123684 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 123684 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 125888 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 125888 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 57311 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 57311 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 155400 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 155400 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 212519 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 215425 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 108745 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 108745 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 108745 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 108745 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 176076 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 176076 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 95641 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 95641 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 103338 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 103338 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 214241 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 95354 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 95354 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 144455 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 144455 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 144455 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 214781 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 4409 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 4409 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 214197 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 210632 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 183795 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 183795 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 214330 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 214091 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 214754 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 103400 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 103400 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 195256 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 195256 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 196134 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 196134 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 196184 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 196184 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 103320 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 103320 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 14176 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 14176 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 14176 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 4409 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 4409 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 120562 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 120562 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 120562 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 66211 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 66211 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 121687 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 121687 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 121687 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 3362 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 3362 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 3362 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 111004 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 111004 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 212569 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 66980 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 66980 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 214286 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 212339 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 85719 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 85719 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 66673 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 66673 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 142089 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 142089 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 142089 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 142089 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 57305 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 57305 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 97720 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 97720 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 168803 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 168803 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 210173 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 210173 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 121405 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 121405 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 121409 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 121409 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 212569 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 213396 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 65704 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 65704 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 214948 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 176634 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 176634 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 176634 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 213327 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 213200 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 210553 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 85710 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 85710 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 215505 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 77595 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 77595 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 163322 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 163322 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 210693 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 90457 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 90457 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 215495 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 103318 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 103318 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 115330 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 115330 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 86833 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 86833 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 86833 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 155439 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 155439 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 111007 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 111007 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 79749 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 79749 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 173061 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 173061 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 103373 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 103373 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 4626 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 4626 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 4626 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 4626 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 212587 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 142089 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 142089 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 142089 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 142089 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 212275 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 212477 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 213907 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 208815 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 208815 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 183965 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 183965 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 215732 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 215680 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 215742 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 14178 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 14178 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 14178 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 214638 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 208814 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 2728 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 2728 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 2728 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 2728 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 212617 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 214002 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 208817 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 208817 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 214726 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 90465 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 90465 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 66276 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 66276 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 210775 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 210775 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 210653 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 166621 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 166621 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 3656 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 3656 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 3656 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 214199 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 125049 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 125049 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 142089 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 142089 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 142089 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 142089 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 121401 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 121401 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 66262 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 66262 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 65446 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 65446 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 171292 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 171292 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 178548 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 178548 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 208813 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 208813 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 57314 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 57314 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 215339 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 66142 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 66142 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 57312 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 57312 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 57547 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 57547 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 3385 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 3385 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 3385 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 2852 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 2852 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 2852 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 214127 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 208814 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 214781 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 214195 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 208515 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 213926 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 212479 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 3930 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 3930 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 3930 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 161042 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 161042 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 99170 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 99170 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 214227 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 111005 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 111005 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 209408 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 121394 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 121394 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 139353 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 139353 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 121686 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 121686 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 121686 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 120552 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 120552 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 120552 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 212591 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 103321 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 103321 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 168714 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 168714 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 174300 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 174300 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 121685 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 121685 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 121685 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 90463 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 90463 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 97479 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 97479 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 161324 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 161324 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 161324 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 173149 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 173149 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 188840 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 188840 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 214282 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 215280 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 115329 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 115329 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 64567 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 64567 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 66179 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 66179 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 191298 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 191298 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 214169 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 214181 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 214181 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 215581 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 189323 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 189323 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 189384 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 189384 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 215581 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 111006 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 111006 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 99107 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 99107 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 97511 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 97511 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 111003 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 111003 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 57313 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 57313 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 214302 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 171062 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 171062 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 178601 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 178601 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 175168 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 175168 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 90464 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 90464 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 86833 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 86833 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 86833 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 215028 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 213103 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 79943 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 79943 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 66308 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 66308 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 215365 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 172137 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 172137 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 2852 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 2852 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 2852 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 189324 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 189324 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 191861 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 191861 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 90467 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 90467 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 112585 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 112585 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 112585 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 214277 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 213910 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 213396 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 178509 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 178509 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 103322 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 103322 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 209538 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 214402 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 213191 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 169833 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 169833 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 214748 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 215352 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 174638 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 174638 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 212803 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 121397 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 121397 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 166404 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 166404 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 2852 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 2852 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 2852 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 111011 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 111011 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 171009 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 171009 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 107901 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 107901 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 161324 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 161324 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 161324 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 189307 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 189307 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 66973 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 66973 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 65701 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 65701 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 99665 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 99665 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 213688 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 90466 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 90466 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 57306 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 57306 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 209530 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 111008 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 111008 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 90461 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 90461 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 90459 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 90459 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 212480 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 111002 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 111002 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 214774 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 214178 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 103340 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 103340 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 98271 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 98271 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 215673 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 158823 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 158823 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 158823 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 215604 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 57307 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 57307 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 214952 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 178435 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 178435 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 4450 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 4450 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 213910 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 14177 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 14177 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 14177 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 90470 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 90470 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 173955 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 173955 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 97484 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 97484 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 209408 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 74053 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 74053 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 1043 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 1043 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 1043 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 178506 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 178506 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 178506 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 178506 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 188817 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 188817 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 178595 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 178595 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 194921 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 194921 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 195759 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 195759 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 187517 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 187517 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 187517 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 187517 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 96685 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 96685 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 96685 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 96685 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 178710 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 178710 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 178710 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 178710 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 178481 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 178481 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 178460 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 178460 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 195775 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 195775 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 178713 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 178713 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 178456 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 178456 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 178657 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 178657 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 178715 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 178715 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 189387 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 189387 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 178467 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 178467 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 178566 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 178566 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 2107 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 2107 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 2107 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 185767 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 185767 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 178591 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 178591 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 96684 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 96684 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 145519 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 145519 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 189454 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 189454 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 91753 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 91753 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 6037 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 6037 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 91797 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 91797 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 154978 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 154978 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 65125 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 65125 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 76663 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 76663 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 62606 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 62606 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 189486 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 189486 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 73661 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 73661 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 76651 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 76651 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 6041 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 6041 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 56432 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 56432 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 56432 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 187239 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 187239 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 186309 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 186309 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 76665 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 76665 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 56432 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 56432 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 56432 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 91232 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 91232 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 139003 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 139003 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 90377 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 90377 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 145180 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 145180 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 64475 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 64475 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 91897 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 91897 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 195043 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 195043 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 65610 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 65610 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 76662 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 76662 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 96216 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 96216 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 122624 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 122624 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 122624 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 122624 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 14022 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 14022 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 14022 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 63459 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 63459 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 170665 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 170665 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 6185 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 6185 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 14030 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 14030 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 14030 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 64886 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 64886 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 90344 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 90344 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 145715 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 145715 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 155696 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 155696 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 65571 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 65571 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 5969 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 5969 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 189380 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 189380 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 79522 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 79522 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 178709 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 178709 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 196240 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 196240 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 187727 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 187727 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 196191 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 196191 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 196701 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 196701 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 178635 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 178635 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 196061 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 196061 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 196428 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 196428 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 96686 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 96686 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 6043 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 6043 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 178733 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 178733 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 158295 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 158295 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 38001 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 38001 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 38201 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 38201 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 147633 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 147633 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 5494 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 5494 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 95896 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 95896 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 95896 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 95896 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 138999 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 138999 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 187498 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 187498 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 78113 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 78113 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 139017 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 139017 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 76656 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 76656 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 138664 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 138664 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 90654 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 90654 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 65268 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 65268 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 123313 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 123313 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 139125 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 139125 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 90628 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 90628 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 186327 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 186327 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 193242 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 193242 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 96218 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 96218 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 5970 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 5970 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 139034 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 139034 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 14023 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 14023 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 14023 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 78709 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 78709 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 156998 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 156998 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 156998 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 156998 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 189175 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 189175 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 195270 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 195270 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 96678 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 96678 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 145518 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 145518 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 56430 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 56430 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 56430 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 56430 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 56430 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 56430 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 90627 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 90627 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 91228 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 91228 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 5873 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 5873 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 138949 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 138949 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 146891 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 146891 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 166396 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 166396 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 178466 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 178466 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 166396 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 166396 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 96217 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 96217 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 56429 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 56429 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 56429 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 56429 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 56429 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 56429 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 145519 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 145519 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 178737 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 178737 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 74353 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 74353 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 178736 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 178736 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 179185 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 179185 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 195635 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 195635 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 196080 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 196080 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 187605 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 187605 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 90626 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 90626 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 178503 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 178503 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 148655 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 148655 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 76664 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 76664 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 133539 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 133539 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 77790 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 77790 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 166396 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 166396 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 91798 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 91798 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 90888 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 90888 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 76661 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 76661 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 5487 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 5487 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 139268 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 139268 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 178622 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 178622 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 187499 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 187499 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 76653 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 76653 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 189443 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 189443 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 5868 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 5868 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 178442 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 178442 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 196523 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 196523 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 2107 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 2107 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 2107 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 189245 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 189245 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 65463 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 65463 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 6184 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 6184 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 139016 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 139016 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 145735 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 145735 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 90343 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 90343 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 139079 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 139079 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 6042 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 6042 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 193366 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 193366 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 178502 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 178502 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 195245 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 195245 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 90654 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 90654 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 56431 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 56431 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 77937 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 77937 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 166396 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 166396 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 139154 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 139154 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 5967 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 5967 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 95958 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 95958 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 178596 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 178596 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 179155 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 179155 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 5900 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 5900 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 178516 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 178516 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 56433 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 56433 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 56433 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 72678 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 72678 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 56433 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 56433 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 56433 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 195764 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 195764 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 145519 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 145519 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 56431 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 56431 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 145562 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 145562 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 90654 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 90654 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 95792 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 95792 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 65014 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 65014 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 145439 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 145439 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 161720 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 161720 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 178455 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 178455 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 96438 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 96438 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 90628 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 90628 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 90623 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 90623 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 139343 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 139343 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 179165 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 179165 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 95791 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 95791 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 6038 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 6038 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 196190 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 196190 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 91231 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 91231 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 90655 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 90655 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 96674 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 96674 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 165891 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 165891 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 129669 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 129669 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 91230 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 91230 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 62651 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 62651 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 210174 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 210174 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 210174 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 56433 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 56433 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 56433 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 62651 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 62651 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 140366 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 140366 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 210777 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 210777 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 140368 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 140368 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 210777 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 1043 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 1043 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 1043 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 140510 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 140510 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 210777 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 140378 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 140378 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 9796 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 9796 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 109665 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 109665 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 9338 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 9338 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 9366 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 9366 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 8683 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 8683 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 110597 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 110597 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 9344 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 9344 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 14176 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 14176 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 14176 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 8728 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 8728 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 108844 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 108844 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 9679 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 9679 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 3852 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 3852 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 3852 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 93145 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 93145 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 2474 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 2474 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 2474 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 3362 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 3362 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 3362 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 3073 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 3554 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 3554 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 3668 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 3668 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 3668 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 3385 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 3385 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 3385 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 877 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 877 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 877 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 877 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 877 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 3547 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 3547 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 3547 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 3238 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 3930 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
3917 3930 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
44430609 3930 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
44430609 3930 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
CHEMBL409969 3930 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
CHEMBL409969 3930 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
16131448 2849 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2849 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2849 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2849 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2849 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2849 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1691 2107 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 2107 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 2107 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 3529 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 3529 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 3529 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 3529 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 3529 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 3529 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 1043 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 1043 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 1043 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 1043 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 1043 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 1043 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 2825 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 2825 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 (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

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weight		 Rot
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CHEMBL414542 213138 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 161853 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 161853 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 210679 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 182055 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 182055 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 212708 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 159840 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 159840 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 213204 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 169405 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 169405 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 210605 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 182027 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 182027 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 183516 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 183516 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 174070 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 174070 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 210632 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 161042 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 161042 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 183326 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 183326 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 180907 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 180907 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 212855 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 180220 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 180220 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 180034 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 180034 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 182727 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 182727 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 213774 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 183398 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 183398 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 210579 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 96501 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 96501 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 213192 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 181844 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 181844 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 212629 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 182599 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 182599 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 182884 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 182884 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 172261 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 172261 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 179417 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 179417 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 210663 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 2852 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 2852 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 2852 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 212550 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 213844 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 180481 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 180481 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 180320 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 180320 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 180031 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 180031 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 180141 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 180141 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 877 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 877 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 877 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 877 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 877 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 181390 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 181390 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 180320 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 180320 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 212995 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 181844 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 181844 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 181815 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 181815 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 210417 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 180141 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 180141 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 210419 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 181438 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 181438 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 183922 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 183922 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 181878 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 181878 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 210417 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 183398 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 183398 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 180203 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 180203 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 180437 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 180437 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 182027 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 182027 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 182329 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 182329 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 4409 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 4409 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 181199 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 181199 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 179699 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 179699 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 180220 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 180220 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 181438 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 181438 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 180681 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 180681 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 180742 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 180742 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 179961 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 179961 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 183516 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 183516 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 183922 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 183922 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 38051 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 38051 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 183051 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 183051 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 180096 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 180096 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 181199 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 181199 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 182934 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 182934 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 181390 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 181390 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 183150 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 183150 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 182727 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 182727 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 182934 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 182934 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 180907 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 180907 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 182599 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 182599 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 183326 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 183326 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 161277 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 161277 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 67756 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 67756 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 181525 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 181525 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 180031 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 180031 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 179790 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 179790 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 180974 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 180974 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 180742 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 180742 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 213137 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 180481 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 180481 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 213067 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 173356 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 173356 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 179675 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 179675 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 181815 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 181815 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 180203 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 180203 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 181129 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 181129 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 179675 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 179675 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 212629 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 213154 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 213687 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 180974 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 180974 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 213103 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 99242 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 99242 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 2852 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 2852 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 2852 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 213139 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 180437 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 180437 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 180034 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 180034 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 182884 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 182884 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 183227 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 183227 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 182055 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 182055 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 182329 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 182329 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 210419 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 179790 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 179790 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 183227 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 183227 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 212995 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 179417 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 179417 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 180681 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 180681 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 183051 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 183051 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 101860 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 101860 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 181878 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 181878 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 182828 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 182828 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 183126 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 183126 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 183126 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 183126 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 181525 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 181525 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 179634 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 179634 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 179634 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 179634 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 175863 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 175863 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 179699 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 179699 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 2852 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 2852 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 2852 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 212818 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 180096 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 180096 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 182828 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 182828 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 183150 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 183150 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 179961 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 179961 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 213518 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 213356 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 181129 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 181129 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 115131 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 115131 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 115131 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 213152 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 115133 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 115133 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 169352 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 169352 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 213926 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 215593 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 467 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 467 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 467 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 214213 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 467 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 467 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 467 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 74053 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 74053 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 215735 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 215743 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 1043 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 1043 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 1043 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 214557 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 210663 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 215732 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 215680 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 215742 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 214127 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 2852 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 2852 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 2852 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 214169 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 214181 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 214195 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 214181 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 214197 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 212617 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 214185 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 178506 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 178506 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 178506 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 178506 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 213739 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 214091 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 176652 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 176652 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 176652 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 97720 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 97720 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 161592 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 161592 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 178635 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 178635 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 178566 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 178566 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 178566 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 178566 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 210775 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 194921 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 194921 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 214178 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 161567 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 161567 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 178715 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 178715 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 214199 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 215657 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 178595 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 178595 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 187727 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 187727 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 189387 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 189387 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 214180 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 215604 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 215626 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 96685 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 96685 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 96685 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 96685 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 212427 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 115132 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 115132 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 178467 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 178467 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 195775 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 195775 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 188817 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 188817 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 196191 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 196191 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 215682 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 115133 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 115133 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 178460 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 178460 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 155439 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 155439 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 96684 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 96684 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 178596 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 178596 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 166621 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 166621 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 178657 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 178657 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 14023 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 14023 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 14023 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 161720 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 161720 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 96678 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 96678 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 72151 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 72151 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 168434 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 168434 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 136008 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 136008 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 140621 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 140621 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 166063 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 166063 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 72299 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 72299 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 135203 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 135203 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 135361 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 135361 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 140893 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 140893 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 72847 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 72847 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 168650 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 168650 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 135259 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 135259 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 133013 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 133013 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 187239 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 187239 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 196384 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 196384 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 212533 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 60577 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 60577 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 60935 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 60935 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 133518 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 133518 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 60915 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 60915 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 60949 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 60949 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 72678 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 72678 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 74438 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 74438 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 195796 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 195796 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 133442 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 133442 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 135207 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 135207 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 96679 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 96679 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 77372 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 77372 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 60937 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 60937 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 212587 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 187525 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 187525 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 215673 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 195850 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 195850 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 72892 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 72892 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 140360 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 140360 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 141308 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 141308 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 72975 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 72975 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 117235 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 117235 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 95641 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 95641 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 97484 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 97484 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 96699 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 96699 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 155650 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 155650 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 78191 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 78191 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 60930 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 60930 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 60946 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 60946 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 60931 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 60931 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 95792 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 95792 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 195043 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 195043 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 195588 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 195588 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 155386 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 155386 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 72498 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 72498 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 178538 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 178538 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 193218 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 193218 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 72840 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 72840 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 133829 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 133829 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 79511 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 79511 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 60948 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 60948 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 60932 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 60932 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 60942 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 60942 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 178622 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 178622 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 97479 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 97479 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 117233 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 117233 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 195526 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 195526 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 196661 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 196661 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 196702 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 196702 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 117232 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 117232 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 95896 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 95896 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 96674 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 96674 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 196538 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 196538 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 95896 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 95896 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 73929 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 73929 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 117242 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 117242 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 193242 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 193242 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 136041 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 136041 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 96022 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 96022 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 60933 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 60933 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 60928 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 60928 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 10049 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 10049 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 196624 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 196624 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 9930 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 9930 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 178442 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 178442 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 195759 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 195759 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 95791 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 95791 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 178591 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 178591 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 215581 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 215581 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 115131 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 115131 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 115131 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 178481 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 178481 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 214002 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 2107 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 2107 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 2107 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 2107 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 2107 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 2107 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 14022 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 14022 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 14022 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 14030 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 14030 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 14030 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 2107 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 2107 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 2107 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 178710 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 178710 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 178710 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 178710 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 178713 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 178713 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 187517 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 187517 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 187517 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 187517 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 168714 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 168714 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 158295 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 158295 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 101860 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 101860 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 101860 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 101860 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 196287 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 196287 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 60944 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 60944 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 60950 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 60950 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 60929 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 60929 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 74202 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 74202 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 178455 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 178455 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 97511 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 97511 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 168893 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 168893 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 195931 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 195931 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 78061 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 78061 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 60947 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 60947 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 213928 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 178427 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 178427 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 3144 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 3144 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 3144 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 72080 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 72080 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 96217 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 96217 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 172750 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 172750 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 74045 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 74045 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 79020 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 79020 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 74401 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 74401 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 156763 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 156763 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 140629 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 140629 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 10065 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 10065 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 60945 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 60945 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 60908 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 60908 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 170274 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 170274 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 117236 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 117236 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 195538 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 195538 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 168318 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 168318 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 189253 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 189253 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 178502 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 178502 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 187500 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 187500 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 210740 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 72530 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 72530 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 189371 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 189371 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 189371 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 189371 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 196098 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 196098 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 60924 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 60924 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 164023 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 164023 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 140296 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 140296 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 73671 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 73671 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 157659 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 157659 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 159453 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 159453 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 213907 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 213667 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 196428 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 196428 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 196701 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 196701 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 95354 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 95354 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 117237 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 117237 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 140577 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 140577 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 2154 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 2154 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 2154 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 60922 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 60922 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 133599 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 133599 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 60940 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 60940 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 60927 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 60927 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 157252 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 157252 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 60923 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 60923 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 133599 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 133599 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 157523 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 157523 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 70269 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 70269 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 60925 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 60925 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 72374 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 72374 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 96673 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 96673 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 196062 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 196062 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 187529 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 187529 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 196111 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 196111 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 74415 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 74415 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 117228 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 117228 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 73938 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 73938 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 111355 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 111355 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 60911 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 60911 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 72193 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 72193 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 166164 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 166164 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 187499 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 187499 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 192726 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 192726 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 73939 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 73939 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 141341 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 141341 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 168790 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 168790 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 117240 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 117240 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 178786 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 178786 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 212339 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 141338 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 141338 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 178503 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 178503 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 9910 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 9910 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 72576 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 72576 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 73010 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 73010 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 212591 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 187605 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 187605 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 117230 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 117230 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 196240 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 196240 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 178456 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 178456 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 161277 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 161277 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 95958 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 95958 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 196190 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 196190 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 213327 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 79522 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 79522 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 117238 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 117238 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 166096 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 166096 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 60941 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 60941 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 79931 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 79931 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 110670 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 110670 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 78383 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 78383 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 79732 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 79732 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 155400 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 155400 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 132741 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 132741 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 78084 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 78084 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 79840 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 79840 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 133539 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 133539 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 168803 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 168803 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 72397 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 72397 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 60910 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 60910 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 60939 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 60939 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 77790 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 77790 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 171833 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 171833 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 60909 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 60909 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 96686 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 96686 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 97834 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 97834 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 178516 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 178516 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 38051 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 38051 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 74028 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 74028 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 60912 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 60912 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 196450 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 196450 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 166282 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 166282 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 195129 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 195129 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 178785 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 178785 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 195395 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 195395 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 165971 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 165971 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 195451 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 195451 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 96218 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 96218 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 60919 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 60919 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 178458 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 178458 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 77494 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 77494 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 78000 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 78000 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 78113 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 78113 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 73516 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 73516 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 79727 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 79727 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 136052 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 136052 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 96216 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 96216 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 195245 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 195245 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 38001 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 38001 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 38201 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 38201 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 178737 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 178737 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 72373 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 72373 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 77373 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 77373 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 141351 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 141351 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 141351 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 141351 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 141351 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 141351 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 138363 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 138363 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 117229 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 117229 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 178474 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 178474 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 187214 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 187214 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 138367 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 138367 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 138664 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 138664 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 139343 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 139343 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 195197 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 195197 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 95868 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 95868 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 60914 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 60914 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 74409 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 74409 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 178655 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 178655 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 60938 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 60938 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 187606 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 187606 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 72083 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 72083 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 189486 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 189486 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 189175 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 189175 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 155599 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 155599 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 196523 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 196523 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 135175 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 135175 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 78709 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 78709 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 60921 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 60921 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 136093 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 136093 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 187530 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 187530 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 193366 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 193366 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 73190 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 73190 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 60936 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 60936 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 72142 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 72142 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 178565 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 178565 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 110638 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 110638 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 60920 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 60920 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 60918 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 60918 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 155696 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 155696 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 60943 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 60943 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 117234 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 117234 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 187498 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 187498 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 74353 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 74353 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 196080 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 196080 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 178712 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 178712 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 115131 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 115131 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 115131 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 195635 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 195635 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 210693 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 117239 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 117239 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 72214 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 72214 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 117241 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 117241 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 60917 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 60917 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 60916 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 60916 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 72240 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 72240 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 38543 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 38543 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 161241 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 161241 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 72456 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 72456 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 73661 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 73661 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 60934 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 60934 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 60913 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 60913 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 195460 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 195460 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 73966 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 73966 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 212562 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 72140 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 72140 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 195270 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 195270 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 178733 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 178733 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 196061 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 196061 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 178736 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 178736 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 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 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 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 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 156998 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 156998 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 156998 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 156998 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 178466 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 178466 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 195764 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 195764 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 140277 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 140277 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 141329 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 141329 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 95794 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 95794 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 169680 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 169680 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 77937 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 77937 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 195777 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 195777 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 139268 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 139268 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 10122 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 10122 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 60926 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 60926 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 117231 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 117231 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 115131 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 115131 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 115131 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 179824 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 179824 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 181135 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 181135 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 179824 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 179824 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 212818 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 181135 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 181135 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 212630 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 212630 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 212818 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 212630 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 212630 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 169405 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 169405 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 213204 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 210632 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 161042 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 161042 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 3930 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 3930 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 3930 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 2728 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 2728 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 2728 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 2728 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 96501 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 96501 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 77602 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 77602 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 212277 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 210579 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 210679 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 213138 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 212274 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 210174 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 213774 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 112689 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 112689 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 112689 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 77607 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 77607 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 112703 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 112703 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 112703 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 57547 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 57547 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 212708 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 120483 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 120483 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 2474 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 2474 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 2474 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 78325 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 78325 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 78325 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 83595 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 83595 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 77605 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 77605 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 112651 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 112651 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 112651 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 110120 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 110120 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 112615 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 112615 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 112615 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 112695 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 112695 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 112695 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 112701 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 112701 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 112701 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 210605 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 208517 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 183922 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 183922 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 120560 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 120560 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 120560 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 120560 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 83598 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 83598 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 2407 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 2407 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 2407 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 2407 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 77380 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 77380 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 77380 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 77380 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 112617 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 112617 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 112617 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 77387 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 77387 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 77387 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 112623 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 112623 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 112623 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 77601 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 77601 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 77603 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 77603 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 159466 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 159466 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 213154 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 142412 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 142412 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 77604 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 77604 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 77589 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 77589 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 77589 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 77589 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 112702 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 112702 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 112702 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 112616 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 112616 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 112616 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 212855 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 183923 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 183923 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 57307 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 57307 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 77593 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 77593 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 78335 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 78335 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 78335 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 112635 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 112635 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 112635 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 77593 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 77593 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 112686 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 112686 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 112686 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 210777 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 183796 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 183796 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 112633 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 112633 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 112633 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 120565 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 120565 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 120565 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 77608 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 77608 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 191209 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 191209 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 7610 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 7610 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 174070 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 174070 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 183944 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 183944 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 77590 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 77590 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 77590 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 77590 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 1043 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 1043 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 1043 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 213103 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 188370 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 188370 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 169222 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 169222 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 78334 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 78334 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 78334 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 3385 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 3385 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 3385 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 3529 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 3529 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 3529 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 3529 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 3529 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 3529 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 208516 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 3547 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 3547 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 3547 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 147184 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 147184 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 174218 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 174218 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 183795 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 183795 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 120560 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 120560 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 120560 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 120560 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 139183 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 139183 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 212751 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 205158 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 205158 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 3529 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 3529 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 3529 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 77594 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 77594 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 208515 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 2852 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 2852 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 2852 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 112645 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 112645 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 112645 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 172261 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 172261 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 161277 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 161277 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 161277 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 161277 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 77606 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 77606 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 210524 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 87367 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 87367 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 179357 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 179357 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 189713 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 189713 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 171128 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 171128 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 120559 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 120559 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 120559 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 2107 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 2107 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 2107 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 3385 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 3385 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 3385 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 212952 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 107043 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 107043 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 77599 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 77599 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 77599 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 185767 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 185767 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 213192 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 194680 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 194680 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 120528 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 120528 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 87751 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 87751 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 87930 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 87930 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 154400 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 154400 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 154749 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 154749 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 169350 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 169350 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 179224 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 179224 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 179306 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 179306 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 179486 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 179486 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 180492 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 180492 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 189816 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 189816 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 145519 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 145519 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 120554 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 120554 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 120554 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 120557 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 120557 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 120557 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 96202 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 96202 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 99170 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 99170 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 67756 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 67756 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 107126 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 107126 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 183965 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 183965 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 212275 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 153616 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 153616 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 214286 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 78637 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 78637 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 120567 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 120567 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 120567 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 2849 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 2849 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 2849 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 2849 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 2849 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 2849 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 85705 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 85705 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 86873 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 86873 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 179115 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 179115 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 189590 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 189590 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 5868 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 5868 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 213382 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 2852 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 2852 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 2852 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 191298 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 191298 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 99170 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 99170 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 112642 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 112642 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 152070 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 152070 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 78634 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 78634 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 99665 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 99665 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 142089 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 142089 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 142089 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 142089 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 87016 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 87016 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 87368 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 87368 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 179117 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 179117 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 180840 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 180840 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 189655 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 189655 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 174600 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 174600 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 6043 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 6043 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 146436 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 146436 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 62651 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 62651 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 57306 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 57306 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 78640 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 78640 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 2852 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 2852 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 2852 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 212427 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 212572 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 179305 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 179305 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 190023 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 190023 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 91210 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 91210 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 170869 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 170869 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 147321 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 147321 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 210775 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 96158 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 96158 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 213002 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 86862 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 86862 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 180300 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 180300 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 189566 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 189566 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 189647 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 189647 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 91132 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 91132 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 2852 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 2852 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 2852 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 120631 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 120631 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 57312 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 57312 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 76665 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 76665 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 212629 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 103400 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 103400 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 85710 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 85710 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 179301 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 179301 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 179358 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 179358 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 91228 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 91228 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 145519 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 145519 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 145519 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 145519 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 148655 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 148655 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 120558 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 120558 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 120558 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 210653 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 213687 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 87548 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 87548 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 186327 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 186327 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 144984 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 144984 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 171655 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 171655 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 120562 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 120562 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 120562 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 120571 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 120571 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 120571 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 125801 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 125801 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 3362 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 3362 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 3362 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 99665 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 99665 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 95913 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 95913 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 78637 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 78637 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 105447 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 105447 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 113991 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 113991 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 147985 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 147985 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 91131 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 91131 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 91131 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 91131 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 7624 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 7624 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 4409 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 4409 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 4409 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 4409 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 99107 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 99107 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 179379 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 179379 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 189571 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 189571 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 98271 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 98271 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 148470 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 148470 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 4409 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 4409 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 4409 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 4409 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 96093 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 96093 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 150135 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 150135 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 57308 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 57308 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 173955 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 173955 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 179481 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 179481 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 166597 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 166597 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 120462 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 120462 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 95970 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 95970 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 143408 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 143408 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 102922 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 102922 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 205072 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 205072 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 153293 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 153293 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 87523 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 87523 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 179977 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 179977 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 173716 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 173716 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 77596 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 77596 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 78638 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 78638 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 78639 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 78639 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 96398 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 96398 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 189324 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 189324 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 179626 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 179626 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 183945 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 183945 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 7558 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 7558 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 96158 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 96158 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 138949 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 138949 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 214444 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 30897 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 30897 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 31806 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 31806 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 168295 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 168295 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 87931 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 87931 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 189171 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 189171 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 212595 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 77599 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 77599 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 77599 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 161032 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 161032 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 86768 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 86768 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 178436 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 178436 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 120552 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 120552 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 120552 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 120455 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 120455 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 210663 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 67756 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 67756 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 96203 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 96203 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 212818 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 151293 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 151293 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 103393 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 103393 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 79943 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 79943 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 115328 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 115328 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 189380 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 189380 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 178662 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 178662 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 189411 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 189411 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 103330 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 103330 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 103336 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 103336 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 103339 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 103339 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 103340 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 103340 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 103343 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 103343 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 205122 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 205122 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 205160 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 205160 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 145562 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 145562 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 120570 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 120570 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 120570 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 96976 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 96976 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 139017 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 139017 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 83594 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 83594 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 175168 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 175168 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 171292 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 171292 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 122624 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 122624 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 91775 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 91775 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 147390 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 147390 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 212630 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 212630 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 212663 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 97781 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 97781 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 178788 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 178788 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 102881 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 102881 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 143695 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 143695 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 142001 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 142001 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 76655 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 76655 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 145519 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 145519 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 152315 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 152315 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 109685 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 109685 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 152924 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 152924 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 208772 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 97702 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 97702 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 115311 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 115311 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 147985 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 147985 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 163351 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 163351 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 110951 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 110951 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 6053 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 6053 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 96833 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 96833 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 148618 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 148618 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 5487 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 5487 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 6875 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 6875 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 62649 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 62649 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 147321 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 147321 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 150620 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 150620 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 64870 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 64870 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 178480 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 178480 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 3903 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 3903 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 3903 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 3903 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 148351 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 148351 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 101718 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 101718 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 65610 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 65610 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 122624 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 122624 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 142116 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 142116 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 86853 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 86853 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 115326 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 115326 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 115340 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 115340 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 179130 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 179130 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 186309 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 186309 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 178514 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 178514 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 178548 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 178548 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 75010 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 75010 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 176214 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 176214 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 6184 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 6184 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 112585 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 112585 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 112585 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 173356 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 173356 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 111008 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 111008 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 80114 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 80114 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 80114 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 90463 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 90463 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 91771 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 91771 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 128177 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 128177 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 76660 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 76660 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 4359 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 4359 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 96157 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 96157 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 31675 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 31675 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 87749 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 87749 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 120553 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 120553 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 120553 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 108529 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 108529 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 96766 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 96766 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 5873 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 5873 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 168311 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 168311 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 5512 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 5512 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 132039 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 132039 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 9163 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 9163 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 78291 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 78291 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 88227 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 88227 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 62647 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 62647 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 144524 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 144524 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 109665 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 109665 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 115301 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 115301 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 135180 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 135180 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 145443 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 145443 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 149439 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 149439 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 169426 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 169426 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 115336 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 115336 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 91718 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 91718 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 8629 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 8629 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 8629 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 8629 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 165891 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 165891 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 97581 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 97581 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 85698 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 85698 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 86767 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 86767 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 115341 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 115341 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 179135 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 179135 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 103341 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 103341 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 189182 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 189182 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 111007 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 111007 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 90344 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 90344 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 147633 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 147633 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 170665 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 170665 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 124335 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 124335 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 120471 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 120471 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 188213 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 188213 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 179145 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 179145 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 90465 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 90465 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 77595 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 77595 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 113939 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 113939 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 32362 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 32362 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 103328 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 103328 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 99349 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 99349 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 99637 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 99637 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 65014 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 65014 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 85709 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 85709 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 69808 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 69808 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 212952 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 143408 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 143408 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 101194 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 101194 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 65463 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 65463 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 9414 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 9414 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 121306 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 121306 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 87824 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 87824 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 76652 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 76652 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 88057 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 88057 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 172163 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 172163 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 85687 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 85687 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 85687 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 85687 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 85687 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 85687 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 178435 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 178435 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 103350 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 103350 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 128197 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 128197 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 34654 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 34654 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 76662 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 76662 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 145443 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 145443 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 2594 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 2594 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 2594 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 2594 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 2594 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 97697 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 97697 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 112866 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 112866 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 150123 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 150123 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 85707 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 85707 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 91719 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 91719 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 65705 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 65705 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 85686 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 85686 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 5253 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 5253 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 111615 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 111615 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 168259 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 168259 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 96006 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 96006 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 86727 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 86727 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 173006 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 173006 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 142483 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 142483 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 107327 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 107327 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 64475 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 64475 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 103381 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 103381 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 85967 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 85967 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 86765 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 86765 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 189423 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 189423 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 91220 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 91220 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 169377 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 169377 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 91772 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 91772 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 178682 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 178682 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 124336 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 124336 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 87521 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 87521 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 121409 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 121409 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 156952 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 156952 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 147263 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 147263 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 67005 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 67005 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 213356 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 153838 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 153838 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 96790 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 96790 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 87017 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 87017 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 147911 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 147911 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 115315 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 115315 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 103321 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 103321 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 103331 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 103331 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 7449 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 7449 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 91797 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 91797 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 148675 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 148675 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 90459 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 90459 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 99803 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 99803 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 4331 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 4331 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 172295 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 172295 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 108551 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 108551 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 213157 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 104888 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 104888 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 189790 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 189790 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 173061 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 173061 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 112867 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 112867 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 175548 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 175548 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 7745 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 7745 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 128190 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 128190 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 110692 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 110692 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 90628 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 90628 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 154635 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 154635 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 128186 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 128186 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 178656 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 178656 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 62650 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 62650 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 65709 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 65709 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 90624 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 90624 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 99099 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 99099 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 153458 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 153458 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 87522 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 87522 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 178549 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 178549 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 103332 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 103332 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 65706 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 65706 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 5899 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 5899 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 77886 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 77886 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 120564 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 120564 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 120564 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 145129 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 145129 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 85739 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 85739 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 144524 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 144524 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 138942 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 138942 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 129040 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 129040 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 86682 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 86682 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 32880 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 32880 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 32880 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 152012 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 152012 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 149592 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 149592 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 115307 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 115307 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 115329 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 115329 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 179129 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 179129 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 103345 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 103345 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 189386 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 189386 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 91297 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 91297 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 83599 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 83599 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 156643 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 156643 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 212803 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 151212 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 151212 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 174389 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 174389 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 210003 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 115320 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 115320 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 129039 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 129039 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 148292 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 148292 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 154189 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 154189 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 128193 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 128193 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 129043 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 129043 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 210553 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 125800 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 125800 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 152636 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 152636 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 103374 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 103374 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 79749 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 79749 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 86602 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 86602 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 179135 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 179135 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 6052 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 6052 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 66973 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 66973 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 139022 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 139022 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 179375 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 179375 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 65703 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 65703 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 90469 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 90469 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 139066 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 139066 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 151231 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 151231 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 97732 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 97732 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 87515 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 87515 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 79111 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 79111 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 5208 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 5208 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 171655 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 171655 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 97456 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 97456 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 156490 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 156490 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 7672 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 7672 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 110962 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 110962 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 66211 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 66211 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 123641 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 123641 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 111011 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 111011 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 85691 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 85691 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 194975 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 194975 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 147720 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 147720 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 85958 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 85958 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 189205 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 189205 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 103335 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 103335 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 91232 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 91232 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 189776 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 189776 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 193421 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 193421 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 141597 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 141597 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 141597 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 213154 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 149202 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 149202 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 152315 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 152315 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 167927 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 167927 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 123070 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 123070 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 128194 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 128194 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 110961 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 110961 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 172462 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 172462 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 178480 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 178480 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 85957 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 85957 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 213053 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 195256 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 195256 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 196184 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 196184 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 79932 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 79932 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 85719 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 85719 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 142089 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 142089 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 142089 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 142089 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 86725 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 86725 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 178602 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 178602 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 91776 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 91776 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 170646 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 170646 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 90654 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 90654 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 91230 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 91230 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 145715 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 145715 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 145735 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 145735 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 166396 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 166396 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 113990 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 113990 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 171833 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 171833 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 57559 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 57559 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 77597 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 77597 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 77597 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 78633 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 78633 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 98271 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 98271 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 179801 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 179801 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 180303 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 180303 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 191861 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 191861 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 111002 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 111002 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 78635 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 78635 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 189738 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 189738 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 169833 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 169833 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 78636 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 78636 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 119003 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 119003 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 212550 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 163175 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 163175 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 86769 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 86769 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 138999 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 138999 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 175357 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 175357 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 176406 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 176406 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 176406 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 116678 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 116678 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 2107 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 2107 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 2107 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 189277 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 189277 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 91289 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 91289 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 179382 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 179382 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 91289 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 91289 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 172971 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 172971 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 6038 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 6038 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 95861 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 95861 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 91791 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 91791 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 139016 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 139016 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 125796 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 125796 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 152687 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 152687 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 98635 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 98635 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 99242 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 99242 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 183830 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 183830 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 5900 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 5900 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 212995 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 96431 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 96431 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 190769 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 190769 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 34000 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 34000 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 148431 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 148431 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 66142 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 66142 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 149031 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 149031 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 178628 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 178628 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 6049 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 6049 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 175261 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 175261 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 99590 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 99590 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 98614 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 98614 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 172395 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 172395 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 6185 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 6185 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 111005 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 111005 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 213137 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 147263 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 147263 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 65125 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 65125 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 115318 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 115318 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 115330 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 115330 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 115331 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 115331 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 186569 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 186569 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 178577 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 178577 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 103318 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 103318 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 91753 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 91753 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 91798 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 91798 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 113990 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 113990 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 35266 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 35266 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 90468 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 90468 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 163166 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 163166 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 176634 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 176634 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 176634 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 108745 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 108745 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 108745 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 108745 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 108745 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 108745 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 125797 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 125797 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 189633 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 189633 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 113890 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 113890 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 151356 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 151356 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 146979 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 146979 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 142412 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 142412 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 97895 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 97895 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 143256 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 143256 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 186308 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 186308 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 6357 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 6357 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 159913 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 159913 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 149108 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 149108 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 115332 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 115332 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 189165 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 189165 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 189165 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 189165 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 189165 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 189165 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 90460 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 90460 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 120976 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 120976 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 137000 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 137000 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 164655 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 164655 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 6287 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 6287 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 176064 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 176064 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 173871 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 173871 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 86681 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 86681 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 63901 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 63901 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 97613 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 97613 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 77599 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 77599 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 77599 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 78676 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 78676 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 103386 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 103386 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 189351 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 189351 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 103324 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 103324 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 65704 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 65704 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 5968 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 5968 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 146891 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 146891 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 128178 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 128178 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 110597 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 110597 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 85699 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 85699 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 91706 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 91706 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 66262 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 66262 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 166281 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 166281 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 5872 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 5872 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 6221 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 6221 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 128182 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 128182 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 66307 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 66307 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 103392 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 103392 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 157403 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 157403 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 142089 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 142089 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 142089 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 142089 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 150997 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 150997 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 153261 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 153261 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 91576 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 91576 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 91576 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 91576 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 90627 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 90627 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 173149 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 173149 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 174553 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 174553 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 148433 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 148433 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 66163 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 66163 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 7467 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 7467 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 180004 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 180004 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 153838 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 153838 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 107265 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 107265 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 65707 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 65707 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 65571 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 65571 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 99290 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 99290 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 103385 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 103385 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 147125 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 147125 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 115310 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 115310 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 179129 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 179129 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 171731 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 171731 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 121401 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 121401 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 115321 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 115321 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 71838 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 71838 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 91127 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 91127 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 123313 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 123313 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 103389 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 103389 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 189341 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 189341 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 96641 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 96641 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 213074 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 153865 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 153865 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 91130 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 91130 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 212866 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 213334 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 213758 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 208121 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 208121 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 7518 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 7518 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 108618 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 108618 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 7529 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 7529 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 7530 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 7530 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 108531 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 108531 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 9198 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 9198 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 161304 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 161304 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 144277 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 144277 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 189766 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 189766 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 121404 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 121404 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 76656 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 76656 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 76657 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 76657 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 90462 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 90462 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 1313 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 1313 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 1313 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 1313 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 97669 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 97669 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 127293 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 127293 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 79722 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 79722 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 79722 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 106765 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 106765 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 168770 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 168770 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 115313 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 115313 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 115324 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 115324 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 172225 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 172225 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 140366 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 140366 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 78447 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 78447 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 103387 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 103387 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 2495 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 2495 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 2495 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 2495 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 62606 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 62606 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 6037 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 6037 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 194993 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 194993 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 66155 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 66155 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 158733 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 158733 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 179165 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 179165 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 63881 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 63881 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 178486 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 178486 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 76659 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 76659 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 103397 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 103397 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 115309 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 115309 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 103322 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 103322 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 6048 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 6048 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 90343 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 90343 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 91416 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 91416 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 4450 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 4450 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 171298 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 171298 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 95891 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 95891 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 139141 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 139141 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 79774 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 79774 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 120563 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 120563 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 120563 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 128188 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 128188 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 146818 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 146818 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 146436 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 146436 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 85685 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 85685 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 5874 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 5874 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 146138 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 146138 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 189205 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 189205 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 96438 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 96438 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 196134 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 196134 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 85727 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 85727 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 143989 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 143989 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 178509 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 178509 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 189206 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 189206 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 189444 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 189444 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 103317 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 103317 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 103344 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 103344 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 103348 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 103348 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 90626 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 90626 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 90628 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 90628 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 90888 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 90888 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 91897 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 91897 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 145518 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 145518 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 76661 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 76661 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 98000 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 98000 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 139034 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 139034 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 111004 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 111004 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 177689 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 177689 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 155009 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 155009 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 98651 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 98651 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 168639 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 168639 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 166701 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 166701 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 178540 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 178540 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 111003 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 111003 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 189245 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 189245 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 176795 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 176795 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 147299 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 147299 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 7519 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 7519 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 95882 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 95882 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 139079 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 139079 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 188840 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 188840 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 189172 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 189172 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 213465 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 179185 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 179185 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 190079 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 190079 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 120569 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 120569 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 120569 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 66142 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 66142 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 159551 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 159551 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 76664 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 76664 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 188354 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 188354 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 96430 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 96430 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 66980 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 66980 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 163322 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 163322 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 90457 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 90457 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 213526 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 103523 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 103523 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 163364 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 163364 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 7730 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 7730 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 186571 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 186571 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 133581 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 133581 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 8948 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 8948 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 107265 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 107265 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 115335 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 115335 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 178578 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 178578 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 103325 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 103325 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 189105 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 189105 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 6042 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 6042 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 76658 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 76658 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 176076 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 176076 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 140502 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 140502 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 148663 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 148663 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 188854 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 188854 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 212676 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 213009 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 213422 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 129669 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 129669 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 128183 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 128183 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 58722 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 58722 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 5325 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 5325 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 85966 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 85966 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 137002 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 137002 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 152070 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 152070 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 66673 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 66673 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 115308 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 115308 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 106767 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 106767 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 7881 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 7881 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 121513 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 121513 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 103398 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 103398 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 87015 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 87015 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 115314 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 115314 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 180489 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 180489 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 121397 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 121397 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 152865 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 152865 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 121397 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 121397 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 151837 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 151837 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 110965 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 110965 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 110965 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 110965 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 66233 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 66233 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 110498 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 110498 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 120890 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 120890 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 85693 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 85693 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 115306 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 115306 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 7433 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 7433 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 128181 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 128181 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 78548 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 78548 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 143992 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 143992 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 66276 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 66276 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 64864 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 64864 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 103346 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 103346 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 91768 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 91768 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 149465 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 149465 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 150123 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 150123 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 9293 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 9293 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 30931 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 30931 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 110445 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 110445 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 64668 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 8 1 5 5.4 CCc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181830 64668 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 8 1 5 5.4 CCc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44451673 168956 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 168956 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 31739 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 31739 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 66892 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 66892 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 153271 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 153271 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 90654 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 90654 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 189411 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 189411 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 153574 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 153574 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 140510 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 140510 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 65014 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 65014 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 178437 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 178437 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 99954 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 99954 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 64886 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 64886 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 115299 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 115299 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 115338 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 115338 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 212276 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 167859 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 167859 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 97949 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 97949 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 142907 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 142907 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 110954 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 110954 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 210595 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 128187 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 128187 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 166396 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 166396 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 139353 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 139353 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 85706 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 85706 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 143253 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 143253 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 115312 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 115312 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 189307 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 189307 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 103319 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 103319 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 90377 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 90377 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 90623 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 90623 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 90628 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 90628 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 90654 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 90654 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 145439 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 145439 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 166396 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 166396 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 128195 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 128195 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 179274 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 179274 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 90654 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 90654 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 168752 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 168752 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 96205 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 96205 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 57311 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 57311 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 57313 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 57313 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 57314 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 57314 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 179155 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 179155 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 189443 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 189443 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 120566 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 120566 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 120566 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 179165 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 179165 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 189242 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 189242 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 120561 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 120561 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 120561 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 77591 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 77591 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 57305 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 57305 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 77591 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 77591 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 87547 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 87547 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 175863 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 175863 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 144985 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 144985 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 58742 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 58742 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 107901 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 107901 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 97743 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 97743 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 7517 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 7517 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 57487 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 57487 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 156397 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 156397 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 158306 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 158306 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 147206 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 147206 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 178631 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 178631 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 189180 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 189180 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 66187 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 66187 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 90470 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 90470 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 139874 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 139874 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 103329 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 103329 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 146293 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 146293 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 77597 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 77597 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 77597 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 85941 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 85941 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 70318 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 70318 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 6009 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 6009 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 86603 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 86603 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 124001 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 124001 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 120271 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 120271 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 125888 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 125888 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 95828 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 95828 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 99178 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 99178 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 135213 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 135213 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 97300 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 97300 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 132489 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 132489 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 97960 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 97960 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 85721 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 85721 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 103342 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 103342 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 140368 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 140368 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 111382 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 111382 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 154189 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 154189 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 125802 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 125802 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 110952 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 110952 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 110952 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 110952 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 110952 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 110952 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 110952 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 110952 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 171062 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 171062 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 87745 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 87745 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 151837 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 151837 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 163196 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 163196 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 98394 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 98394 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 142088 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 142088 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 127395 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 127395 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 97004 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 97004 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 5967 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 5967 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 121407 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 121407 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 169845 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 169845 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 67056 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 67056 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 106762 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 106762 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 128180 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 128180 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 5898 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 5898 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 88202 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 88202 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 88058 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 88058 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 33105 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 33105 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 33105 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 168972 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 168972 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 66179 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 66179 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 30756 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 30756 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 96727 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 96727 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 110966 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 110966 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 143640 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 143640 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 103388 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 103388 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 103333 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 103333 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 140378 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 140378 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 166396 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 166396 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 179250 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 179250 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 121405 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 121405 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 6220 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 6220 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 5513 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 5513 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 87366 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 87366 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 143588 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 143588 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 180638 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 180638 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 62648 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 62648 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 5511 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 5511 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 7735 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 7735 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 179038 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 179038 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 145808 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 145808 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 148351 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 148351 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 172868 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 172868 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 103373 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 103373 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 103376 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 103376 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 85701 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 85701 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 144728 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 144728 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 115302 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 115302 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 189144 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 189144 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 5970 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 5970 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 90655 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 90655 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 91231 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 91231 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 145180 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 145180 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 65446 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 65446 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 204864 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 204864 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 77600 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 77600 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 189323 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 189323 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 7548 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 7548 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 90466 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 90466 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 189462 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 189462 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 77386 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 77386 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 83597 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 83597 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 143217 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 143217 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 179034 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 179034 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 113989 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 113989 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 120555 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 120555 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 120555 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 87932 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 87932 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 7559 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 7559 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 80294 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 80294 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 80294 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 139154 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 139154 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 76651 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 76651 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 99539 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 99539 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 128199 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 128199 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 77592 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 77592 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 77592 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 77592 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 107222 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 107222 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 139003 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 139003 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 191729 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 191729 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 125797 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 125797 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 172431 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 172431 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 171490 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 171490 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 95921 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 95921 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 96060 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 96060 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 148979 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 148979 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 115319 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 115319 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 115337 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 115337 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 116535 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 116535 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 1664 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 1664 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 1664 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 1664 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 1664 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 210644 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 66977 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 66977 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 123771 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 123771 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 153840 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 153840 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 79107 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 79107 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 97997 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 97997 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 86766 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 86766 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 186721 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 186721 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 128198 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 128198 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 65748 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 65748 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 78007 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 78007 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 78007 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 63459 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 63459 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 138381 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 138381 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 120406 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 120406 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 128189 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 128189 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 150087 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 150087 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 85697 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 85697 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 189751 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 189751 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 149387 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 149387 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 153271 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 153271 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 101736 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 101736 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 85728 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 85728 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 126389 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 126389 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 97701 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 97701 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 148684 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 148684 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 115300 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 115300 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 139064 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 139064 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 103347 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 103347 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 180641 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 180641 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 121402 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 121402 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 121403 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 121403 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 128200 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 128200 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 168462 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 168462 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 146138 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 146138 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 77656 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 77656 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 189585 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 189585 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 5227 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 5227 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 121408 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 121408 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 7732 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 7732 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 115316 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 115316 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 191191 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 191191 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 62644 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 62644 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 62645 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 62645 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 128192 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 128192 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 154975 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 154975 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 85737 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 85737 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 66872 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 66872 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 148208 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 148208 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 103382 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 103382 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 85720 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 85720 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 115303 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 115303 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 115327 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 115327 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 189454 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 189454 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 178601 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 178601 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 178787 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 178787 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 103323 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 103323 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 103338 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 103338 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 107292 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 107292 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 154978 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 154978 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 107292 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 107292 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 66142 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 66142 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 97432 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 97432 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 91129 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 91129 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 33225 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 33225 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 33225 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 5494 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 5494 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 31049 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 31049 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 90464 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 90464 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 57309 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 57309 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 158976 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 158976 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 213139 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 179307 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 179307 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 99498 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 99498 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 91808 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 91808 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 91808 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 91808 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 65604 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 65604 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 62646 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 62646 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 171702 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 171702 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 59337 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 59337 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 129041 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 129041 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 66308 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 66308 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 91209 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 91209 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 128185 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 128185 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 85939 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 85939 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 139948 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 139948 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 88226 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 88226 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 115323 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 115323 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 7547 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 7547 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 121406 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 121406 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 145694 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 145694 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 65592 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 65592 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 133440 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 133440 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 128184 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 128184 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 147206 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 147206 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 64567 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 64567 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 128176 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 128176 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 213165 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 97028 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 97028 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 149136 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 149136 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 110500 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 110500 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 174300 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 174300 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 172673 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 172673 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 128175 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 128175 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 9325 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 9325 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 179225 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 179225 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 166354 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 166354 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 65708 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 65708 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 115322 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 115322 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 87750 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 87750 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 168823 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 168823 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 178629 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 178629 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 115334 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 115334 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 172868 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 172868 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 129042 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 129042 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 5215 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 5215 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 109179 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 109179 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 103380 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 103380 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 70622 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 70622 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 9099 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 9099 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 97470 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 97470 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 31225 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 31225 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 103395 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 103395 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 115304 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 115304 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 115317 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 115317 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 189465 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 189465 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 103320 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 103320 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 103337 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 103337 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 141669 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 141669 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 141669 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 6041 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 6041 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 59160 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 59160 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 97408 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 97408 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 99561 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 99561 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 178445 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 178445 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 77597 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 77597 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 77597 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 144497 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 144497 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 189304 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 189304 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 120549 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 120549 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 120549 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 125049 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 125049 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 4626 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 4626 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 4626 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 4626 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 178539 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 178539 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 90458 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 90458 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 5969 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 5969 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 95922 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 95922 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 115333 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 115333 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 195304 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 195304 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 208406 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 208406 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 79942 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 79942 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 124652 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 124652 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 110213 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 110213 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 106764 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 106764 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 85738 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 85738 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 103326 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 103326 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 145129 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 145129 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 5186 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 5186 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 148402 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 148402 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 115339 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 115339 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 97668 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 97668 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 5424 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 5424 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 103327 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 103327 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 110965 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 110965 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 140702 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 140702 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 151139 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 151139 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 111009 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 111009 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 32989 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 32989 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 32989 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 64458 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 64458 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 189165 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 189165 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 189165 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 189165 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 189165 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 189165 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 143588 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 143588 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 5196 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 5196 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 125516 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 125516 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 120568 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 120568 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 120568 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 100619 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 100619 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 5255 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 5255 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 103349 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 103349 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 121395 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 121395 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 96968 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 96968 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 121395 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 121395 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 121502 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 121502 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 189384 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 189384 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 177690 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 177690 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 71897 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 71897 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 2154 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 2154 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 2154 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 2154 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 2154 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 2154 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 178513 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 178513 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 65268 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 65268 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 91777 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 91777 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 65701 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 65701 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 99530 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 99530 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 139125 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 139125 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 111006 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 111006 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 174802 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 174802 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 90467 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 90467 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 97950 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 97950 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 128179 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 128179 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 121399 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 121399 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 144509 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 144509 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 121399 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 121399 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 57310 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 57310 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 138944 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 138944 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 139552 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 139552 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 95963 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 95963 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 120556 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 120556 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 120556 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 66105 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 66105 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 85692 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 85692 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 115305 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 115305 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 165054 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 165054 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 138421 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 138421 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 121400 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 121400 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 80225 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 80225 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 80225 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 99505 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 99505 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 91720 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 91720 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 110643 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 110643 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 179226 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 179226 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 123684 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 123684 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 62652 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 62652 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 65939 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 65939 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 168814 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 168814 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 168814 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 179479 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 179479 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 87514 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 87514 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 34941 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 34941 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 144810 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 144810 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 9345 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 9345 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 9345 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 9345 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 79013 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 79013 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 119229 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 119229 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 112868 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 112868 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 99328 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 99328 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 189711 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 189711 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 128191 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 128191 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 213191 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 144810 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 144810 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 103375 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 103375 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 103394 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 103394 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 85711 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 85711 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 161748 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 161748 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 103334 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 103334 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 166862 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 166862 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 169000 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 169000 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 125799 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 125799 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 83596 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 83596 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 77598 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 77598 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 120550 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 120550 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 120550 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 172137 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 172137 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 95807 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 95807 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 154750 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 154750 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 169537 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 169537 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 76663 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 76663 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 90461 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 90461 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 153293 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 153293 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 97946 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 97946 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 64844 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 64844 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 189389 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 189389 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 95912 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 95912 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 87348 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 87348 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 98010 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 98010 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 149470 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 149470 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 9162 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 9162 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 108694 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 108694 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 79954 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 79954 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 149136 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 149136 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 153840 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 153840 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 156190 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 156190 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 67222 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 67222 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 136015 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 136015 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 121394 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 121394 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 207657 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 207657 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 121394 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 121394 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 877 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 877 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 877 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 877 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 877 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 141535 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 141535 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 115325 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 115325 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 153039 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 153039 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 151164 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 151164 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 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
16131448 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1681 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1688 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
44361543 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
56947112 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
CHEMBL396460 2849 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1685 3929 0 None - 1 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15509719
23383556 179357 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 179357 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 189713 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 189713 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 179224 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 179224 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 179306 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 179306 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 179486 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 179486 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 180492 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 180492 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 189816 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 189816 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 179115 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 179115 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 189590 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 189590 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 179117 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 179117 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 180840 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 180840 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 189655 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 189655 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 179305 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 179305 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 190023 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 190023 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 180300 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 180300 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 189566 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 189566 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 189647 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 189647 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 179301 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 179301 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 179358 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 179358 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 91131 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 91131 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 179379 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 179379 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 189571 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 189571 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 179481 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 179481 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 179977 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 179977 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 179626 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 179626 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 189171 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 189171 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 216305 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 217472 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 217474 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 217475 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 217476 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 188213 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 188213 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 179145 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 179145 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 189790 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 189790 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 179375 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 179375 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 189776 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 189776 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 179801 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 179801 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 180303 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 180303 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 189738 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 189738 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 175357 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 175357 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 91289 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 91289 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 179382 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 179382 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 190769 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 190769 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 175261 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 175261 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 189633 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 189633 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 91576 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 91576 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 180004 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 180004 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 189766 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 189766 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 177689 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 177689 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 176795 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 176795 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 189172 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 189172 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 190079 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 190079 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 188354 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 188354 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 189105 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 189105 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 180489 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 180489 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 179274 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 179274 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 217473 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 189242 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 189242 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 179250 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 179250 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 180638 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 180638 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 189144 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 189144 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 179034 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 179034 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 1664 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 1664 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 1664 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 1664 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 1664 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 189751 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 189751 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 180641 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 180641 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 189585 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 189585 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 1664 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 1664 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 1664 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 1664 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 1664 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 179307 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 179307 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 91808 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 91808 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 179225 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 179225 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 216002 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 2594 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 2594 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 2594 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 2594 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 2594 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 177690 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 177690 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 174802 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 174802 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 179226 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 179226 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 179479 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 179479 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 189711 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 189711 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 2474 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 2474 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 2474 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 3668 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 3668 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 3668 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 3554 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 3554 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 508 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 508 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 508 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 3547 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 3547 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 3547 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 877 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 3547 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 3547 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 3547 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 3547 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 3547 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 3547 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 2407 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 2407 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 2407 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 2407 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 2407 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 2407 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 2407 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 2407 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 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
16131448 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
16131448 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1681 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1681 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1681 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1688 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1688 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1688 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
44361543 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
44361543 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
44361543 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
56947112 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
56947112 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
56947112 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
CHEMBL396460 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL396460 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL396460 2849 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1694 3928 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
25081457 3928 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1682 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1682 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1682 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1682 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
6324645 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
6324645 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
6324645 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
6324645 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
CHEMBL384755 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL384755 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL384755 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL384755 2852 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
8865 3238 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24903280
1686 3073 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1686 3073 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15743186
50922685 734 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 734 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 2107 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 2107 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 2107 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 509 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 509 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 3529 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 3529 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 3529 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 3529 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 3529 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 3529 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 3362 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 3362 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 3362 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 3362 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 3362 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 3362 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 3385 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 3385 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 3385 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 1043 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 1043 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 1043 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 2719 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 2719 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 2719 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 2719 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 2719 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 2853 0 None - 1 Human 10.4 pKi None 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1696 3051 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
5311338 3051 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
1692 2154 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 2154 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 2154 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 2875 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 1636 0 None - 1 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
16131448 2849 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2849 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2849 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2849 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2849 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2849 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
16143911 467 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
1689 467 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
CHEMBL505874 467 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863