Ligand source activities (1 row/activity)



Get vendors


Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
25208097 183340 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 183340 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 3867 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 3867 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 3867 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 207075 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 207075 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 208887 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 161304 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 161304 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 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1681 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1688 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
44361543 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
56947112 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
CHEMBL396460 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
16131448 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 2806 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44388461 159293 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 159293 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 97414 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 97414 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 97414 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 2806 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 2806 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 2806 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 2806 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 2806 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2806 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL409204 211004 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 208779 6 None - 1 Human 9.8 pEC50 = 9.8 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL2372052 208429 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 2806 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1681 2806 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1688 2806 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
44361543 2806 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
56947112 2806 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL396460 2806 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL265801 208918 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 2806 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1681 2806 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1688 2806 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44361543 2806 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
56947112 2806 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
CHEMBL396460 2806 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44388466 96054 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 96054 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 211255 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 210825 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 207068 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 211634 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 168839 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 168839 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 2809 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
6324645 2809 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 2809 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL1631909 207069 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 207069 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 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1681 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1688 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
44361543 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
56947112 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
CHEMBL396460 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
12419 2439 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 2439 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 2439 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
16131448 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1681 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1688 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44361543 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
56947112 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL396460 2806 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44388462 161304 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 161304 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 208834 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 183340 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 183340 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 2809 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
6324645 2809 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL384755 2809 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
3917 3867 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 3867 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 3867 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 211778 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 207073 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 207073 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 3867 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 3867 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 3867 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 206775 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 159293 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 159293 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 211406 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 2809 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
6324645 2809 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2809 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
16131448 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL507847 212785 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 207075 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 211717 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 168839 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 168839 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 161304 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 161304 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16143911 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL511107 213817 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
1689 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 2806 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1682 2809 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
6324645 2809 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 2809 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
44388461 159293 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 159293 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 2806 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL506825 212442 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 183214 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 183214 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 120054 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 120054 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 120054 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 213958 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 213966 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 190615 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 190615 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 210848 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 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
16131448 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1681 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1688 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
44361543 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
56947112 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 2806 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL1162358 206774 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 183341 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 183341 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 183362 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 183362 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 187786 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 187786 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 77241 19 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 77241 19 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL5073561 212528 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 208887 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 211991 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 212473 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 212919 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 213631 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 212414 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 208789 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 90038 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 90038 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 212673 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 178002 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 178002 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 90027 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 90027 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 212162 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 212409 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 213906 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 2806 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 2806 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 2806 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 2806 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 2806 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 2806 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 2809 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 2809 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 2809 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
76324308 102842 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 102842 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 2806 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 2806 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 2806 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 2806 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 2806 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 2806 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 2809 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 2809 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 2809 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
10406239 120049 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 120049 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 120049 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 120049 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 65375 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 65375 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 212845 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 212162 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 142721 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 142721 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 188576 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 188576 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 188576 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 169278 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 169278 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 85300 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 85300 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 108064 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 108064 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 206664 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 206664 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 212756 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 213881 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 65811 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 65811 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 3491 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 3491 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 3491 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
49843555 57010 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 57010 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 212022 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 211960 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 119977 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 119977 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 210680 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
1679 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11956680 120047 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 120047 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 120047 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 173646 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 173646 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
9803475 77242 22 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 77242 22 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL5087383 213317 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 110520 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 110520 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 114815 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 114815 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 90037 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 90037 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 114816 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 114816 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 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL389521 210680 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 183363 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 183363 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 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
16131448 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL5086442 213256 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 168206 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 168206 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 56134 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 56134 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 208899 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 14005 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 14005 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 14005 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 178210 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 178210 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 90031 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 90031 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 175832 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 175832 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 175832 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 65811 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 65811 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 56134 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 56134 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 177974 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 177974 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 120881 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 120881 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 102872 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 102872 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 143922 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 143922 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 143922 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 208428 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 208428 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 120885 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 120885 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 2806 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2806 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2806 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2806 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2806 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2806 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
9848990 188576 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 188576 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 188576 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 213850 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 14064 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 14064 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 14064 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 210680 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 99078 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 99078 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 212975 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 173981 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 173981 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 114805 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 114805 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 211919 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 121170 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 121170 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 121170 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 65856 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 65856 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 177861 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 177861 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 178052 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 178052 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 106738 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 106738 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 209005 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 210754 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 65824 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 65824 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 168970 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 168970 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
122179061 120892 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 120892 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 65832 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 65832 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 188688 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 188688 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 123167 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 123167 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 125367 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 125367 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 57013 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 57013 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 154861 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 154861 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 210772 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 213650 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 108258 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 108258 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 108258 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 108258 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 175502 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 175502 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 95197 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 95197 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 102863 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 102863 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 212470 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 94910 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 94910 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 143922 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 143922 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 143922 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 213009 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 4343 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 4343 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL505824 212426 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 208887 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 183213 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 183213 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 212559 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 212320 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 212982 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 102925 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 102925 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 193586 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 193586 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 194460 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 194460 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 194510 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 194510 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 102845 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 102845 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 14061 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 14061 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 14061 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 4343 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 4343 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
9925137 120051 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 120051 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 120051 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 65879 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 65879 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 121173 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 121173 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 121173 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 3310 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 3310 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 3310 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
16131448 2806 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
86279209 110515 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 110515 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 210822 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 66646 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 66646 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 212515 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 210592 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 85292 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 85292 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 66340 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 66340 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 141557 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 141557 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 141557 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 141557 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 57007 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 57007 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 97271 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 97271 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 168238 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 168238 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 208428 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 208428 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 120891 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 120891 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 120895 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 120895 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 210822 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 211648 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 65373 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 65373 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 2806 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1681 2806 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1688 2806 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
44361543 2806 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
56947112 2806 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 2806 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL5085090 213175 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 176060 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 176060 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 176060 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 2806 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL424934 211579 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 211452 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 208808 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 85283 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 85283 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 213729 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 77242 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
CHEMBL2088036 77242 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
10042904 162771 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 162771 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 208948 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 90026 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 90026 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 213719 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 102843 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 102843 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 114831 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 114831 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 86405 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 86405 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 86405 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 154900 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 154900 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 110518 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 110518 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 79339 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 79339 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 172492 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 172492 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 102898 8 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 102898 8 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
11461888 4558 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 4558 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
11461888 4558 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 4558 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL405948 210840 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 141557 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 141557 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 141557 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 141557 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 210528 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 210730 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 212159 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 207072 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 207072 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 183383 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 183383 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 213955 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 213904 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 213965 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 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44551464 14063 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 14063 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 14063 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 212866 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 207071 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 2688 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
3829 2688 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
5497186 2688 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL567175 2688 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL406718 210870 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 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2806 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL455289 212249 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 207074 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 207074 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 212954 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 90034 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 90034 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 65944 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 65944 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 209030 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 209030 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 208908 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 166068 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 166068 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 3599 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
53 3599 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL300555 3599 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL505873 212428 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 124529 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 124529 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 141557 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 141557 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 141557 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 141557 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 120887 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 120887 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 65930 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 65930 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 65115 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 65115 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 170726 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 170726 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 177973 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 177973 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 2806 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2806 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2806 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2806 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2806 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2806 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1631920 207070 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 207070 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 57016 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 57016 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 213565 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 65811 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 65811 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 57014 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 57014 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 57243 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 57243 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 3333 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 3333 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 3333 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 2809 15 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
6324645 2809 15 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL384755 2809 15 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL500773 212356 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 207071 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 213009 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 212424 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 206773 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 212178 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 210732 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 3867 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 3867 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 3867 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 160495 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 160495 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 98713 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 98713 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 212456 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 110516 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 110516 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 207663 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 120880 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 120880 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 138823 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 138823 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 121172 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 121172 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 121172 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 120041 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 120041 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 120041 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 210844 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 102846 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 102846 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 168149 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 168149 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 173728 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 173728 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 121171 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 121171 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 121171 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 90032 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 90032 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 97030 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 97030 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 160777 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 160777 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 160777 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 172578 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 172578 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 188253 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 188253 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 212511 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 213506 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 114830 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 114830 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 64236 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 64236 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 65848 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 65848 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 2806 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
1681 2806 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
1688 2806 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
44361543 2806 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
56947112 2806 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2806 22 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
16131448 2806 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
1681 2806 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
1688 2806 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
44361543 2806 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
56947112 2806 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2806 22 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
16131448 2806 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
25207946 190704 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 190704 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 212398 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 212410 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 212410 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 213805 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 188734 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 188734 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 188795 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 188795 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 213805 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 110517 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 110517 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 98650 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 98650 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 97062 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 97062 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 110514 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 110514 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 57015 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 57015 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 212531 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 170495 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 170495 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 178026 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 178026 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 174596 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4570328 174596 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
71624270 90033 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 90033 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 86405 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 86405 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 86405 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 213255 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 211355 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 79533 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 79533 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 65976 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 65976 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 213591 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 171571 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 171571 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 2809 15 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
6324645 2809 15 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL384755 2809 15 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
11848793 188735 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 188735 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 191265 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 191265 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 90036 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 90036 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 112091 7 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3301613 112091 7 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325959 112091 7 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL5072270 212506 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 212162 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 211648 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 177934 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 177934 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 102847 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 102847 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 207793 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 212631 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 211443 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 2806 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1681 2806 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1688 2806 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
44361543 2806 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
56947112 2806 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
CHEMBL396460 2806 22 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
129188454 169266 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 169266 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 212976 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 213578 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 174066 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 174066 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 211056 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 120883 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 120883 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 165851 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 165851 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 2809 15 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
6324645 2809 15 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2809 15 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
90655978 110522 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 110522 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 170442 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 170442 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 107415 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 107415 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 160777 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 160777 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 160777 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 188718 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 188718 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 66639 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 66639 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 65370 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 65370 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 99204 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 99204 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 2806 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1681 2806 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1688 2806 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
44361543 2806 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
56947112 2806 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL396460 2806 22 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL436819 211940 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 90035 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387196 90035 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
53324890 57008 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 57008 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 2806 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2806 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2806 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2806 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2806 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2806 22 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL233069 207785 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 110519 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 110519 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 90030 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 90030 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 90028 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 90028 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 210733 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 110513 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 110513 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 213002 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 212407 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 102865 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 102865 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 97819 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 97819 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 213897 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 158277 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 158277 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 158277 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 213828 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 57009 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 57009 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 213179 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 177860 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 177860 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 4384 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 4384 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 212162 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 14062 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 14062 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 14062 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 90039 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 90039 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 173383 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 173383 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 97035 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 97035 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 207663 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 2806 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2806 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2806 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2806 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2806 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2806 22 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11511090 73705 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 73705 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 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
7361 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL201945 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
44143431 177931 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 177931 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 177931 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 177931 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 188230 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 188230 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 178020 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 178020 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 193252 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 193252 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 194086 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 194086 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 186934 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 186934 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 186934 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 186934 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 96237 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 96237 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 96237 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 96237 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 178133 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 178133 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 178133 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 178133 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 177906 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 177906 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 177885 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 177885 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 194102 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 194102 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 178136 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 178136 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 177881 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 177881 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 178081 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 178081 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 178138 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 178138 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 188798 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 188798 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 177892 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 177892 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 177991 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 177991 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 2076 14 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
5311194 2076 14 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
CHEMBL357076 2076 14 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
24894426 185185 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 185185 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 178016 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 178016 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 96236 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 96236 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 144986 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 144986 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 188864 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 188864 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 91321 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 91321 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 5960 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 5960 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 91365 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 91365 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 154439 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 154439 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 64794 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 64794 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 76310 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 76310 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 62277 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 62277 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 188896 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 188896 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 73314 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 73314 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 76298 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 76298 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 5964 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 5964 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 56138 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 56138 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 56138 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 186656 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 186656 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 185727 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 185727 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 76312 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 76312 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 56138 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 56138 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 56138 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 90801 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 90801 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 138474 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 138474 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 89946 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 89946 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 144647 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 144647 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 64144 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 64144 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 91465 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 91465 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 193373 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 193373 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 65279 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 65279 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 76309 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 76309 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 95769 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 95769 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 122109 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 122109 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 122109 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 122109 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 13908 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 13908 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 13908 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 63129 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 63129 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 170098 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 170098 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 6108 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 6108 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 13916 3 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197275 13916 3 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL564840 13916 3 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44391157 64555 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 64555 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 89913 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 89913 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 145182 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 145182 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 155155 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 155155 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 65240 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 65240 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 5892 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 5892 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 188791 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 188791 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 79112 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 79112 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 178132 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 178132 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 194566 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 194566 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 187144 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 187144 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 194517 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 194517 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 195026 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 195026 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 178059 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 178059 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 194387 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 194387 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 194754 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 194754 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 96238 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 96238 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 5966 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 5966 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 178156 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 178156 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 157750 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 157750 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 37768 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 37768 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 37967 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 37967 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 147100 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 147100 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 5420 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 5420 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 95452 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 95452 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 95452 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 95452 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 138470 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 138470 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 186915 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 186915 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 77759 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 77759 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 138488 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 138488 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 76303 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 76303 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 138135 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 138135 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 90223 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 90223 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 64937 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 64937 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 122797 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 122797 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 138595 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 138595 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 90197 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 90197 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 185745 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 185745 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 192639 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 192639 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 95771 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 95771 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 5893 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 5893 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 138505 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 138505 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 13909 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 13909 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 13909 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 78299 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 78299 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 156456 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 156456 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 156456 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 156456 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 188586 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 188586 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 193600 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 193600 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 96230 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 96230 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 144985 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 144985 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 56136 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 56136 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 56136 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 56136 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 56136 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 56136 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 90196 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 90196 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 90797 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 90797 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 5796 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 5796 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 138420 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 138420 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 146358 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 146358 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 165843 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 165843 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 177891 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 177891 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 165843 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 165843 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 95770 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 95770 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 56135 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 56135 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 56135 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 56135 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 56135 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 56135 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 144986 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 144986 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 178160 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 178160 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 74004 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 74004 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 178159 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 178159 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 178606 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 178606 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 193962 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 193962 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 194406 1 None 1584 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560667 194406 1 None 1584 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143419 187022 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 187022 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 90195 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 90195 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 177928 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 177928 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 148123 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 148123 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 76311 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 76311 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 133016 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 133016 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 77437 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 77437 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 165843 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 165843 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 91366 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 91366 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 90457 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 90457 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 76308 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 76308 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 5413 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 5413 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 138738 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 138738 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 178046 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 178046 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 186916 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 186916 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 76300 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 76300 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 188853 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 188853 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 5791 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 5791 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 177867 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 177867 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 194848 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 194848 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 2076 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
5311194 2076 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
CHEMBL357076 2076 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
11152739 188656 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 188656 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 65132 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 65132 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 6107 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 6107 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 138487 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 138487 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 145202 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 145202 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 89912 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 89912 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 138549 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 138549 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 5965 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 5965 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 192763 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 192763 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 177927 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 177927 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 193575 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 193575 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 90223 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 90223 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 56137 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 56137 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 77583 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 77583 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 165843 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 165843 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 138624 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 138624 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 5890 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 5890 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 95512 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 95512 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 178021 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 178021 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 178576 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 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 178576 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 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 5823 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 5823 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 177941 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 177941 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 56139 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 56139 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 56139 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 72333 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 72333 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 56139 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 56139 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 56139 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 194091 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 194091 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 144986 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 144986 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 56137 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 56137 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 145029 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 145029 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 90223 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 90223 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 95348 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 95348 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 64683 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 64683 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 144906 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 144906 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 161171 0 None 407 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
CHEMBL413571 161171 0 None 407 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
44143445 177880 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 177880 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 95991 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 95991 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 90197 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 90197 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 90192 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 90192 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 138813 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 138813 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 178586 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 178586 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 95347 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 95347 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 5961 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 5961 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 194516 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 194516 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 90800 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 90800 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 90224 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 90224 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 96226 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263889 96226 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44390989 165338 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 165338 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 129147 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 129147 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 90799 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 90799 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 62322 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 62322 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 208429 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 208429 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 208429 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 56139 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 56139 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 56139 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 62322 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 62322 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 139836 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 139836 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 209032 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 209032 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 139838 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 139838 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 209032 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 1027 20 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
7361 1027 20 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL201945 1027 20 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
127043559 139980 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 139980 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 209032 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 139848 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 139848 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 9703 2 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL113684 9703 2 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
11743914 109177 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 109177 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 9248 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 9248 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 9276 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 9276 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 8595 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 8595 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 110108 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 110108 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 9254 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 9254 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 14061 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 14061 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 14061 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 8640 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 8640 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 108357 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 108357 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 9587 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 9587 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 3791 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 3791 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 3791 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 92713 29 None 1 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 None
CHEMBL2443262 92713 29 None 1 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 None
12419 2439 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
24800108 2439 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
CHEMBL481512 2439 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
1684 3310 17 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
9844019 3310 17 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
CHEMBL2088034 3310 17 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
1686 3024 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 15743186
1679 266 21 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
9963005 266 21 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
CHEMBL437723 266 21 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
11597355 3498 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 3498 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 3611 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 3611 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 3611 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 3333 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 3333 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 3333 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 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 864 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8868 3491 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3491 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3491 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
8865 3187 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 24903280
1680 267 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
3917 3867 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
3917 3867 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
44430609 3867 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
44430609 3867 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
CHEMBL409969 3867 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
CHEMBL409969 3867 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
16131448 2806 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2806 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2806 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2806 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2806 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2806 22 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1691 2076 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
5311194 2076 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
CHEMBL357076 2076 14 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
10047612 3473 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
10047612 3473 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1693 3473 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
1693 3473 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
CHEMBL559569 3473 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
CHEMBL559569 3473 14 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
10296561 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
10296561 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
7361 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
7361 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
CHEMBL201945 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
CHEMBL201945 1027 20 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
10500 2783 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 2783 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


Get vendors


Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
CHEMBL414542 211390 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 161304 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 161304 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 208934 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 181473 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 181473 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 210961 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 159293 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 159293 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 211456 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 168839 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 168839 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 208860 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 181445 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 181445 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 182934 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 182934 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 173498 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 173498 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 208887 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 160495 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 160495 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 182744 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 182744 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 2806 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1681 2806 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1688 2806 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
44361543 2806 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
56947112 2806 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
CHEMBL396460 2806 22 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
162656512 180325 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 180325 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 211108 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 179640 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 179640 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 179454 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 179454 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 182145 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 182145 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 212026 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 182816 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 182816 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 208834 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 96054 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 96054 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 211444 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 2806 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 2806 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 2806 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 2806 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 2806 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2806 22 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
162661740 181262 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 181262 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 210882 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 182017 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 182017 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 182302 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 182302 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 171695 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 171695 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 178837 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 178837 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 208918 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 2809 15 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
6324645 2809 15 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL384755 2809 15 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL405212 210803 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 212096 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 179899 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 179899 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 179740 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 179740 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 179451 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 179451 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 179561 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 179561 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 864 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 864 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 864 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3545616 864 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 864 45 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
162659015 180808 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 180808 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 179740 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 179740 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 211248 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 181262 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 181262 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 181233 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 181233 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 208672 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 179561 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 179561 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 208674 16 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2013.05.064
11137032 180856 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 180856 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 183340 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 183340 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 181296 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 181296 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 208672 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 182816 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 182816 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 179623 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 179623 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 179856 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 179856 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 181445 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 181445 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 181747 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 181747 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 4343 12 None 21 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL101454 4343 12 None 21 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
162659601 180617 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 180617 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 179119 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 179119 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 179640 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 179640 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 180856 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 180856 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 180099 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 180099 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 180160 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 180160 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 179381 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 179381 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 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 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 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 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 183340 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 183340 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 37818 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 37818 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 182469 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 182469 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 179516 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 179516 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 180617 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 180617 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 182352 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 182352 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 180808 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 180808 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 182568 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 182568 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 182145 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 182145 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 182352 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 182352 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 180325 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 180325 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 182017 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 182017 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 182744 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 182744 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 160730 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 160730 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 67414 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 67414 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 180943 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 180943 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 179451 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 179451 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 179210 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 179210 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 180392 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 180392 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 180160 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 180160 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 211389 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 179899 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 179899 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 211319 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 172784 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 172784 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 179095 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 179095 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 181233 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 181233 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 179623 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 179623 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 180547 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 180547 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 179095 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 179095 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 210882 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 211406 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 211939 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 180392 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 180392 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 211355 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 98785 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 98785 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 2809 15 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
6324645 2809 15 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
CHEMBL384755 2809 15 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
CHEMBL414543 211391 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 179856 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 179856 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 179454 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 179454 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 182302 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 182302 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 182645 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 182645 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 181473 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 181473 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 181747 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 181747 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 208674 16 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxoneActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxone
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2013.05.064
162648962 179210 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 179210 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 182645 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 182645 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 211248 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 178837 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 178837 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 2806 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
1681 2806 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
1688 2806 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
44361543 2806 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
56947112 2806 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
CHEMBL396460 2806 22 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
162655432 180099 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 180099 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 182469 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 182469 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 101390 16 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
CHEMBL300616 101390 16 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
162661631 181296 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 181296 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 182246 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 182246 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 182544 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 182544 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 182544 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 182544 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 180943 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 180943 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 179054 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 179054 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 179054 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 179054 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 175290 4 None 213 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assay
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4585935 175290 4 None 213 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assay
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
162646448 179119 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 179119 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 2809 15 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
6324645 2809 15 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL384755 2809 15 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL410396 211071 16 None 1 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650635 179516 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 179516 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 182246 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 182246 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 182568 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 182568 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 179381 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 179381 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 211770 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 211608 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 180547 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 180547 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 114633 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 114633 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 114633 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 211404 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 114635 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 114635 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 168786 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 168786 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 2806 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2806 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2806 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2806 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2806 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2806 22 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL443591 212178 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 213817 0 None - 0 Rat 9.8 pIC50 = 9.8 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL506825 212442 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
1689 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 464 14 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 2806 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
11511090 73705 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 73705 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 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL556388 213958 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 213966 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 1027 20 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
7361 1027 20 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL201945 1027 20 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL507847 212785 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 208918 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 2806 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
1681 2806 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
1688 2806 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
44361543 2806 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
56947112 2806 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
CHEMBL396460 2806 22 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
CHEMBL555757 213955 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 213904 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 213965 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 212356 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 2809 15 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
6324645 2809 15 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 2809 15 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
CHEMBL503512 212398 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 212410 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 212424 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 212410 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 212426 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 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL406718 210870 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 212414 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 177931 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 177931 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 177931 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 177931 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 211991 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 212320 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 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
155569742 176078 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 176078 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 176078 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 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2806 22 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
16131448 2806 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44456296 97271 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 97271 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 2806 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1679 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
9963005 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
CHEMBL437723 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
44416444 161044 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 161044 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1604 53 23 20 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
1679 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 266 21 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44143437 178059 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 178059 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 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44143433 177991 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 177991 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 177991 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 177991 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 209030 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 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
45273531 193252 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 193252 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 212407 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 161019 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 161019 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 178138 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 178138 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 212428 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 213881 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 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1679 266 21 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
9963005 266 21 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL437723 266 21 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44143456 178020 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 178020 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 187144 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 187144 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 188798 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 188798 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 212409 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 213828 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 213850 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 96237 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 96237 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 96237 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 96237 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 210680 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 2806 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
1681 2806 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
1688 2806 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
44361543 2806 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
56947112 2806 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
CHEMBL396460 2806 22 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
118717442 114634 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 114634 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 177892 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 177892 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 194102 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 194102 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 188230 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 188230 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 194517 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 194517 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 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1681 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1688 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44361543 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
56947112 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL396460 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL526352 213906 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 114635 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 114635 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 177885 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 177885 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 154900 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 154900 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 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1681 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1688 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44361543 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
56947112 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL396460 2806 22 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44450085 96236 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 96236 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 178021 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 178021 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 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44456185 166068 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 166068 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 178081 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 178081 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 13909 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 13909 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 13909 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 161171 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
CHEMBL413571 161171 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
22272974 96230 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 96230 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 71807 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 71807 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 167870 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 167870 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 135485 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 135485 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 140090 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 140090 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 165510 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 165510 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 71955 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 71955 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 134680 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 134680 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 134838 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 134838 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 140362 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 140362 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 72502 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 72502 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 168085 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 168085 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 134736 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 134736 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 132492 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 132492 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 186656 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 186656 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 194710 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 194710 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 210786 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 60253 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 60253 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 60610 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 60610 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 132995 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 132995 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 60590 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 60590 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 60624 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 60624 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 72333 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 72333 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 74089 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 74089 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 194123 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 194123 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 132921 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 132921 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 134684 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 134684 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 96231 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 96231 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 77019 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 77019 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 60612 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 60612 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 210840 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 186942 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 186942 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 213897 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 194177 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 194177 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 72547 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 72547 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 139830 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 139830 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 140777 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 140777 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 72629 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 72629 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 116732 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 116732 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 95197 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 95197 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 97035 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 97035 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 96251 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 96251 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 155110 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 155110 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 77824 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 77824 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 60605 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 60605 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 60621 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 60621 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 60606 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 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 60606 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 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 95348 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 95348 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 193373 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 193373 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 193915 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 193915 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 154847 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 154847 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 72153 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 72153 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 177963 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 177963 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 192615 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 192615 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 72495 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 72495 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 133306 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 133306 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 79101 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 79101 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 60623 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 60623 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 60607 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 60607 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 60617 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 60617 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 178046 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 178046 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 97030 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 97030 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 116730 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 116730 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 193853 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 193853 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 194986 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 194986 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 195027 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 195027 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 116729 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 116729 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 95452 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 95452 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 96226 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263889 96226 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
45268356 194863 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 194863 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 95452 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 95452 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 73581 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 73581 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 116739 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 116739 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 192639 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 192639 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 135518 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 135518 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 95576 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 95576 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 60608 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 60608 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 60603 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 60603 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 9954 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 9954 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 194949 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 194949 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 9837 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 9837 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 177867 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 177867 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 194086 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 194086 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 95347 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 95347 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 178016 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 178016 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 213805 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 213805 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 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
1681 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
1688 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
44361543 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
56947112 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
CHEMBL396460 2806 22 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
24882570 114633 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 114633 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 114633 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 177906 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 177906 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 212249 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 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
5311194 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
CHEMBL357076 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
1691 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
5311194 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
CHEMBL357076 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
44189834 13908 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 13908 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 13908 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 13916 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197275 13916 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL564840 13916 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
1691 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
5311194 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
CHEMBL357076 2076 14 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
44143432 178133 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 178133 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 178133 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 178133 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 178136 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 178136 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 186934 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 186934 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 186934 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 186934 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 168149 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 168149 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 157750 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 157750 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 101390 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]-Tyr14 at nociceptin (NOP) receptorAbility to displace [125I]-Tyr14 at nociceptin (NOP) receptor
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.09.068
CHEMBL300616 101390 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]-Tyr14 at nociceptin (NOP) receptorAbility to displace [125I]-Tyr14 at nociceptin (NOP) receptor
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.09.068
416359 101390 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
CHEMBL300616 101390 16 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
45267616 194613 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 194613 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 60619 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 60619 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 60625 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 60625 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 60604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 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 60604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 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 73854 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 73854 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 177880 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 177880 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 97062 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 97062 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 168327 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 168327 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 194257 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 194257 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 77707 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 77707 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 60622 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 60622 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 212180 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 177852 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 177852 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 3095 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
6918468 3095 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
CHEMBL41547 3095 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
11710187 71736 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 71736 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 95770 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 95770 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 172181 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 172181 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 73697 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 73697 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 78610 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 78610 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 74052 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 74052 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 156222 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 156222 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 140098 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 140098 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 9970 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 9970 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 60620 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 60620 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 60583 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 60583 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 169707 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 169707 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 116733 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 116733 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 193865 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 193865 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 167755 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 167755 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 188664 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 188664 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 177927 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 177927 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 186917 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 186917 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 208995 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 72185 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 72185 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 188782 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 188782 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 188782 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 188782 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 194424 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 194424 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 60599 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 60599 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 163471 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 163471 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 139766 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 139766 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 73323 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 73323 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 157117 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 157117 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 158906 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 158906 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 212159 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 211919 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 194754 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 194754 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 195026 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 195026 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 94910 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 94910 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 116734 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 116734 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 140047 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 140047 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 2123 23 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
5311340 2123 23 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
CHEMBL140979 2123 23 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
52916714 60597 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 60597 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 133076 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 133076 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 60615 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 60615 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 60602 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 60602 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 156710 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 156710 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 60598 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 60598 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 133076 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 133076 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 156981 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 156981 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 69926 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 69926 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 60600 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 60600 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 72029 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 72029 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 96225 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 96225 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 194388 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 194388 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 186946 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 186946 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 194437 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 194437 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 74066 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 74066 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 116725 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 116725 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 73590 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 73590 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 110867 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 110867 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 60586 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 60586 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 71849 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 71849 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 165611 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 165611 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 186916 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 186916 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 192124 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 192124 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 73591 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 73591 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 140810 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 140810 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 168225 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 168225 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 116737 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 116737 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 178209 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 178209 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 210592 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 140807 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 140807 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 177928 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 177928 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 9817 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 9817 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 72231 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 72231 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 72664 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 72664 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 210844 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 187022 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 187022 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 116727 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 116727 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 194566 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 194566 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 177881 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 177881 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 160730 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 160730 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 95512 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 95512 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 194516 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 194516 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 211579 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 79112 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 79112 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 116735 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 116735 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 165543 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 165543 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 60616 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 60616 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 79521 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 79521 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 110181 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 110181 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 77980 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 77980 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 79322 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 79322 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 154861 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 154861 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 132220 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 132220 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 77730 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 77730 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 79430 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 79430 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 133016 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 133016 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 168238 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 168238 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 72052 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 72052 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 60585 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 60585 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 60614 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 60614 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 77437 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 77437 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 171267 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 171267 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 60584 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 60584 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 96238 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 96238 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 97385 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 97385 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 177941 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 177941 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 37818 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 37818 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 73680 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 73680 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 60587 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 60587 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 194776 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 194776 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 165729 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 165729 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 193459 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 193459 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 178208 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 178208 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 193724 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 193724 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 165418 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 165418 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 193780 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 193780 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 95771 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 95771 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 60594 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 60594 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 177883 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 177883 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 77141 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 77141 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 77646 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 77646 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 77759 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 77759 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 73169 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 73169 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 79317 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 79317 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 135529 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 135529 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 95769 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 95769 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 193575 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 193575 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 37768 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 37768 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 37967 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 37967 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 178160 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 178160 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 72028 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 72028 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 77020 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 77020 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 140820 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 140820 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 140820 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 140820 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 140820 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 140820 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 137835 4 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
CHEMBL377140 137835 4 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
118726261 116726 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 116726 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 177899 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 177899 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 186631 7 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 367 5 1 5 4.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL492396 186631 7 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 367 5 1 5 4.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
11372671 137839 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 137839 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 138135 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 138135 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 138813 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 138813 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 193527 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 193527 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 95424 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 95424 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 60589 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 60589 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 74060 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 74060 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 178079 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 178079 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 60613 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 60613 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 187023 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 187023 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 71739 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 71739 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 188896 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 188896 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 188586 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 188586 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 155059 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 155059 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 194848 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 194848 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 134652 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 134652 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 78299 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 78299 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 60596 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 60596 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 135570 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 135570 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 186947 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 186947 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 192763 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 192763 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 72843 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 72843 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 60611 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 60611 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 71798 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 71798 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 177990 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 177990 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 110149 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 110149 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 60595 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 60595 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 60593 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 60593 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 155155 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 155155 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 60618 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 60618 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 116731 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 116731 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 186915 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 186915 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 74004 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 74004 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 194406 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560667 194406 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143426 178135 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 178135 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 114633 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 114633 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 114633 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 193962 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 193962 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 208948 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 116736 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 116736 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 71870 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 71870 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 116738 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 116738 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 60592 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 60592 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 60591 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 60591 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 71896 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 71896 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 38307 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 CCn1c(=O)n([C@H]2CCN(CC3CCCCCCC3)C[C@@H]2CO)c2ccccc21 10.1021/jm990517p
CHEMBL146462 38307 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 CCn1c(=O)n([C@H]2CCN(CC3CCCCCCC3)C[C@@H]2CO)c2ccccc21 10.1021/jm990517p
44449850 160694 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 160694 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 72111 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 72111 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 73314 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 73314 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 60609 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 60609 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 60588 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 60588 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 193789 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 193789 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 73618 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 73618 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 210815 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 71796 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 71796 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 193600 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 193600 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 178156 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 178156 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 194387 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 194387 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 178159 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 178159 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 178132 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 178132 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 156456 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 156456 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 156456 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 156456 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 177891 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 177891 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 194091 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 194091 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 139747 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 139747 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 140798 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 140798 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 95350 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 95350 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 169113 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 169113 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 77583 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 77583 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 194104 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 194104 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 138738 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 138738 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 10027 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 10027 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 60601 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 60601 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 116728 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 116728 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 2806 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1681 2806 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1688 2806 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
44361543 2806 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
56947112 2806 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
CHEMBL396460 2806 22 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
16131448 2806 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 2806 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 2806 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 2806 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 2806 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 2806 22 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
16131448 2806 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2806 22 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
24882570 114633 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 114633 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 114633 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 179244 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 179244 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 180553 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 180553 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 179244 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 179244 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 211071 16 None 1 2 Human 7.8 pKd = 7.8 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657543 180553 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 180553 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 210883 16 None 2 2 Human 7.5 pKd = 7.5 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406946 210883 16 None 2 2 Human 7.5 pKd = 7.5 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410396 211071 16 None 1 2 Human 8.2 pKd = 8.2 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10654047 210883 16 None 2 2 Human 7.1 pKd = 7.1 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406946 210883 16 None 2 2 Human 7.1 pKd = 7.1 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
44388467 168839 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 168839 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 211456 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 208887 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 160495 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 160495 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 3867 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 3867 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 3867 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 2688 6 None 2 11 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 2688 6 None 2 11 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 2688 6 None 2 11 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 2688 6 None 2 11 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 96054 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 96054 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 77249 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 77249 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 210530 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 208834 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 2806 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
1681 2806 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
1688 2806 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
44361543 2806 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
56947112 2806 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2806 22 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
CHEMBL266191 208934 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 211390 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 210527 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 208429 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 212026 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 2806 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
1681 2806 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
1688 2806 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
44361543 2806 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
56947112 2806 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
CHEMBL396460 2806 22 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
68182754 112192 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 112192 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 112192 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 77254 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 77254 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 112206 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 112206 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 112206 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 57243 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 57243 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 210961 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 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1681 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1688 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
44361543 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
56947112 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL396460 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
9842289 119977 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 119977 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 2439 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 2439 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 2439 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
58268629 77922 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 77922 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 77922 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 83182 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 83182 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 77252 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 77252 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 112154 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 112154 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 112154 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 109631 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 109631 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 112118 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 112118 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 112118 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 112198 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 112198 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 112198 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 112204 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 112204 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 112204 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 208860 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 2806 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
1681 2806 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
1688 2806 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
44361543 2806 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
56947112 2806 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 2806 22 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
CHEMBL1162359 206775 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 183340 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 183340 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 120049 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 120049 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 120049 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 120049 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 83185 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 83185 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 2375 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
9462 2375 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
CHEMBL3304244 2375 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
DB16048 2375 28 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
52951807 77027 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 77027 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 77027 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 77027 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 112120 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 112120 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 112120 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 77034 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 77034 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 77034 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 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
68182789 112126 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 112126 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 112126 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 77248 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 77248 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 77250 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 77250 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 158919 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 158919 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 211406 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 141880 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 141880 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 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
1681 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
1688 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
44361543 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
56947112 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
CHEMBL396460 2806 22 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
70697391 77251 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 77251 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 77236 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088029 77236 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951808 77236 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 77236 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 112205 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 112205 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 112205 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 112119 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 112119 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 112119 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 211108 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 183341 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 183341 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 57009 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 57009 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 77240 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 77240 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 77932 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 77932 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 77932 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 112138 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 112138 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 112138 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 77240 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 77240 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 112189 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 112189 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 112189 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 209032 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 183214 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 183214 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 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
58268591 112136 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 112136 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 112136 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 120054 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 120054 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 120054 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 77255 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 77255 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 190615 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 190615 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 7529 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 7529 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 173498 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 173498 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 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
1681 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
1688 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
44361543 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
56947112 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
CHEMBL396460 2806 22 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
25208245 183362 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 183362 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 77237 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 77237 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 77237 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 77237 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 1027 20 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
7361 1027 20 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL201945 1027 20 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL413944 211355 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 187786 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 187786 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 168656 0 None 13 3 Rat 9.6 pKi = 9.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL440928 168656 0 None 13 3 Rat 9.6 pKi = 9.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
70691173 77931 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 77931 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 77931 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 3333 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 3333 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 3333 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 3473 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
1693 3473 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
CHEMBL559569 3473 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
10047612 3473 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
1693 3473 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
CHEMBL559569 3473 14 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
CHEMBL1162358 206774 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 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1681 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1688 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
44361543 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
56947112 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
CHEMBL396460 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
8868 3491 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 3491 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 3491 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
44438983 146651 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 146651 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 173646 0 None 7 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 173646 0 None 7 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
25207948 183213 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 183213 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 120049 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 120049 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 120049 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 120049 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 138653 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 138653 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 211004 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 203447 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 203447 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 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2806 22 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
10047612 3473 14 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
1693 3473 14 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL559569 3473 14 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
11464846 77241 19 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 77241 19 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL1162357 206773 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 2809 15 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
6324645 2809 15 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2809 15 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
58268645 112148 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 112148 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 112148 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 171695 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 171695 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 160730 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 160730 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 160730 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 160730 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 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
1681 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
1688 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
44361543 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
56947112 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
16131448 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 2806 22 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
60154200 77253 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 77253 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 208779 6 None - 1 Mouse 9.4 pKi = 9.4 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44430038 86939 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 86939 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 178777 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 178777 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 189121 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 189121 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 170562 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 170562 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 120048 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 120048 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 120048 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 2076 14 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
5311194 2076 14 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
CHEMBL357076 2076 14 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
15512229 3333 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 3333 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 3333 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 211205 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 106560 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 106560 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 77246 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 77246 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 77246 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 185185 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 185185 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 211444 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 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1681 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1688 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44361543 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
56947112 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL396460 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44297539 193014 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 193014 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 120017 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 120017 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 87323 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 87323 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 87502 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 87502 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 153866 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 153866 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 154211 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 154211 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 168784 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 168784 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 178645 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 178645 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 178726 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 178726 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 178906 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 178906 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 179910 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 179910 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 189224 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 189224 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 144986 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 144986 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 120043 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 120043 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 120043 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 120046 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 120046 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 120046 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 95755 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 95755 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 98713 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 98713 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 67414 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 67414 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 106642 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 106642 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 183383 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 183383 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 210528 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 153082 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 153082 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 212515 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 78227 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 78227 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 120056 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 120056 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 120056 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 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1681 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1688 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44361543 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
56947112 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL396460 2806 22 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44426832 85278 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 85278 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 86445 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 86445 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 178536 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 178536 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 188999 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 188999 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 5791 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 5791 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 211634 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 2809 15 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
6324645 2809 15 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2809 15 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
25207946 190704 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 190704 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 98713 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 98713 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 112145 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 112145 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 151538 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 151538 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 78224 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 78224 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 99204 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 99204 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 141557 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 141557 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 141557 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 141557 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 86588 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 86588 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 86940 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 86940 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 178538 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 178538 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 180258 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 180258 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 189063 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 189063 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 174028 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 174028 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 5966 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 5966 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 145903 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 145903 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 62322 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 62322 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 57008 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 57008 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 78230 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 78230 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 2809 15 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
6324645 2809 15 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
CHEMBL384755 2809 15 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
CHEMBL389521 210680 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 210825 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 178725 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 178725 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 189430 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 189430 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 90779 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 90779 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 170302 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 170302 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 146788 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 146788 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 209030 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 95711 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 95711 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 211255 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 86434 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 86434 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 179720 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 179720 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 188975 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 188975 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 189055 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 189055 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 90701 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 90701 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 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
11848225 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3545616 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
1682 2809 15 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
6324645 2809 15 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 2809 15 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
10000890 120119 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 120119 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 57014 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 57014 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 76312 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 76312 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 210882 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 102925 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 102925 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 85283 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 85283 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 178721 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 178721 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 178778 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 178778 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 90797 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 90797 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 144986 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 144986 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 144986 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 144986 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 148123 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 148123 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 120047 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 120047 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 120047 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 208908 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 211939 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 87120 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 87120 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 185745 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 185745 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 144451 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 144451 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 171089 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 171089 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 120051 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 120051 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 120051 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 120060 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 120060 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 120060 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 125280 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 125280 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 3310 17 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 3310 17 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 3310 17 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9997843 99204 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 99204 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 95467 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 95467 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 78227 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 78227 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 104968 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 104968 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 113492 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 113492 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 147452 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 147452 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 90700 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 90700 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 90700 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 90700 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 7543 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 7543 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 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
9905428 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
10714523 98650 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 98650 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 178799 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 178799 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 188980 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 188980 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 97819 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 97819 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 147938 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 147938 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 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL101454 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
9905428 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL101454 4343 12 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
44451918 95647 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 95647 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 149602 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 149602 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 57010 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 57010 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 173383 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 173383 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 178901 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 178901 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 166044 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 166044 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 119956 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 119956 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 95524 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 95524 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 142876 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 142876 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 102449 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 102449 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 203363 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 203363 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 152759 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 152759 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 87095 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 87095 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 179397 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 179397 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 173144 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 173144 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 77243 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 77243 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 78228 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 78228 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 78229 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 78229 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 95951 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 95951 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 188735 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 188735 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 179046 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 179046 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 183363 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 183363 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 7477 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 7477 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 95711 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 95711 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 138420 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 138420 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 212673 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 30681 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 30681 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 31590 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 31590 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 167732 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 167732 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 87503 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 87503 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 188582 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 188582 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 210848 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 77246 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 77246 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 77246 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 160485 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 160485 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 86341 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 86341 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 177861 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 177861 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 120041 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 120041 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 120041 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 119949 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 119949 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 208918 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 67414 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 67414 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 95756 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 95756 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 211071 16 None -1 2 Mouse 8.0 pKi = 8 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
44252685 150761 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 150761 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 102918 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 102918 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 79533 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 79533 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 114829 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 114829 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 188791 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 188791 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 178086 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 178086 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 188822 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 188822 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 102855 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 102855 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 102861 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 102861 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 102864 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 102864 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 102865 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 102865 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 102868 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 102868 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 203412 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 203412 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 203449 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 203449 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 145029 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 145029 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 120059 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 120059 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 120059 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 96528 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 96528 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 138488 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 138488 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 83181 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 83181 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 174596 0 None 54 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4570328 174596 0 None 54 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
134563466 170726 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 170726 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 122109 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 122109 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 91343 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 91343 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 146857 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 146857 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 210883 16 None -2 2 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL406946 210883 16 None -2 2 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL407461 210916 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 97332 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 97332 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 178211 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 178211 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 102408 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 102408 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 143163 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 143163 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 141469 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 141469 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 76302 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 76302 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 144986 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 144986 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 151783 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 151783 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 109197 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 109197 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 152391 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 152391 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 207030 17 None -3388 2 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmcl.2006.05.060
24799325 97253 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 97253 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 114812 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 114812 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 147452 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 147452 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 162799 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 162799 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 110462 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 110462 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 5976 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 5976 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 96385 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 96385 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 148086 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 148086 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 5413 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 5413 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 6797 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 6797 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 62320 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 62320 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 146788 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 146788 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 150087 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 150087 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 64539 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 64539 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 177905 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 177905 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 3840 36 None -776 10 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 3840 36 None -776 10 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 3840 36 None -776 10 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 3840 36 None -776 10 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 147819 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 147819 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 101248 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 101248 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 65279 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 65279 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 122109 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 122109 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 141584 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 141584 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 86425 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 86425 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 114827 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 114827 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 114841 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 114841 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 178551 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 178551 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 185727 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 185727 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 177939 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 177939 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 177973 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 177973 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 74660 42 None 17 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 321 3 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL203356 74660 42 None 17 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 321 3 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
155569552 175640 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 175640 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 6107 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 6107 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 112091 7 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3301613 112091 7 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325959 112091 7 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
155544763 172784 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 172784 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 110519 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 110519 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 79704 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 79704 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 79704 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 90032 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 90032 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 91339 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 91339 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 127655 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 127655 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 76307 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 76307 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 4293 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 4293 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 95710 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 95710 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 31460 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 31460 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 87321 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 87321 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 120042 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 120042 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 120042 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 108042 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 108042 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 96318 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 96318 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 5796 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 5796 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 167748 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 167748 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 5437 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 5437 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 131517 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 131517 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 9073 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 9073 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 77890 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 77890 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 87799 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 87799 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 62318 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 62318 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 143991 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 143991 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 109177 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 109177 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 114802 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 114802 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 134657 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 134657 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 144910 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 144910 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 148907 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 148907 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 168859 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 168859 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 114837 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 114837 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 91286 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 91286 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 8542 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 8542 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 8542 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 8542 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 165338 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 165338 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 97132 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 97132 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 85271 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 85271 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 86340 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 86340 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 114842 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 114842 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 178556 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 178556 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 102866 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 102866 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 188593 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 188593 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 110518 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 110518 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 89913 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 89913 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 147100 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 147100 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 170098 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 170098 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 123816 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 123816 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 119965 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 119965 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 187630 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 187630 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 178566 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 178566 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 90034 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 90034 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 77242 22 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 77242 22 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
12986256 113440 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 113440 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 32146 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 32146 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 102853 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 102853 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 98890 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 98890 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 99176 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 99176 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 64683 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 64683 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 85282 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 85282 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 69465 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 69465 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 211205 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 142876 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 142876 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 100724 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 100724 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 65132 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 65132 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 9324 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 9324 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 120792 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 120792 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 87396 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 87396 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 76299 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 76299 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 87629 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 87629 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 171597 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 171597 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 85260 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 85260 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 85260 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 85260 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 85260 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 85260 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 177860 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 177860 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 102875 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 102875 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 127675 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 127675 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 34431 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 34431 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 76309 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 76309 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 144910 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 144910 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 2556 18 None -5 12 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 2556 18 None -5 12 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 2556 18 None -5 12 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 2556 18 None -5 12 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 2556 18 None -5 12 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 97248 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 97248 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 112368 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 112368 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 149590 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 149590 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 85280 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 85280 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 91287 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 91287 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 65374 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 65374 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 85259 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 85259 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 5182 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 5182 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 111125 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 111125 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 167696 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 167696 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 95560 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 95560 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 86300 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 86300 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 172437 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 172437 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 141951 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 141951 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 106843 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 106843 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 64144 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 64144 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 102906 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 102906 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 85540 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 85540 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 86338 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 86338 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 188833 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 188833 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 90789 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 90789 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 168811 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 168811 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 91340 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 91340 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 178106 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 178106 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 123817 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 123817 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 87093 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 87093 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 120895 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 120895 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 156410 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 156410 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 146730 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 146730 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 66670 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 66670 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 211608 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 153304 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 153304 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 96342 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 96342 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 86589 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 86589 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 147378 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 147378 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 114816 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 114816 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 102846 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 102846 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 102856 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 102856 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 7368 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 7368 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 91365 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 91365 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 148143 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 148143 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 90028 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 90028 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 99342 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 99342 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 4265 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 4265 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 171729 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 171729 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 108064 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 108064 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 211409 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 104409 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 104409 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 189198 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 189198 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 172492 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 172492 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 112369 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 112369 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 174975 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 174975 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 7663 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 7663 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 127668 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 127668 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 110203 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 110203 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 90197 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 90197 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 154098 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 154098 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 127664 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 127664 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 178080 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 178080 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 62321 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 62321 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 65378 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 65378 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 90193 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 90193 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 98642 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 98642 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 152924 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 152924 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 87094 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 87094 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 177974 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 177974 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 102857 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 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 102857 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 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 65375 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 65375 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 5822 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 5822 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 77533 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 77533 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 120053 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 120053 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 120053 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 144596 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 144596 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 85312 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 85312 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 143991 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 143991 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 138413 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 138413 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 128518 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 128518 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 86255 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 86255 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 32661 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 32661 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 32661 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 151480 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 151480 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 149060 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 149060 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 114808 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 114808 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 114830 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 114830 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 178550 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 178550 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 102870 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 102870 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 188797 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 188797 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 90866 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 90866 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 83186 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 83186 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 156102 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 156102 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 211056 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 150680 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 150680 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 173817 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 173817 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 208258 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 114821 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 114821 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 128517 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 128517 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 147760 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 147760 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 153655 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 153655 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 127671 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 127671 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 128521 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 128521 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 208808 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 125279 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 125279 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 152104 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 152104 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 102899 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 102899 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 79339 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 79339 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 86175 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 86175 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 178556 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 178556 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 5975 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 5975 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 66639 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 66639 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 138493 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 138493 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 178795 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 178795 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 65372 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 65372 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 90038 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 90038 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 138537 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 138537 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 150699 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 150699 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 97283 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 97283 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 87087 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 87087 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 78701 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 78701 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 5137 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 5137 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 171089 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 171089 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 97007 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 97007 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 155949 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 155949 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 7591 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 7591 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 110473 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 110473 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 65879 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 65879 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 123124 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 123124 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 110522 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 110522 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 85264 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 85264 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 193305 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 193305 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 147187 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 147187 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 85531 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 85531 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 188616 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 188616 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 102860 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 102860 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 90801 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 90801 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 189184 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 189184 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 192818 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 192818 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 141065 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 141065 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 141065 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 211406 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 148670 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 148670 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 151783 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 151783 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 167364 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 167364 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 122554 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 122554 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 127672 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 127672 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 110472 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 110472 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 171895 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 171895 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 177905 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 177905 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 85530 74 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 267 3 1 2 3.2 OC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230141 85530 74 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 267 3 1 2 3.2 OC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL413178 211305 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 193586 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 193586 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 194510 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 194510 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 79522 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 79522 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 85292 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 85292 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 141557 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 141557 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 141557 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 141557 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 86298 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 86298 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 178027 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 178027 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 91344 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 91344 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 170079 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 170079 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 90223 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 90223 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 90799 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 90799 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 145182 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 145182 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 145202 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 145202 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 165843 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 165843 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 113491 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 113491 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 171267 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 171267 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 57255 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 57255 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 77244 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 77244 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 77244 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 78223 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 78223 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 97819 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 97819 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 179221 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 179221 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 179723 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 179723 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 191265 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 191265 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 110513 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 110513 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 78225 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 78225 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 189146 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 189146 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 169266 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 169266 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 78226 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 78226 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 118498 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL342580 118498 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL405212 210803 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 162625 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 162625 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 86342 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 86342 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 138470 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 138470 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 174785 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 174785 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 175832 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 175832 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 175832 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 116178 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 428 6 2 6 4.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc([N+](=O)[O-])cc3)ccc2n1 10.1021/jm0002073
CHEMBL337128 116178 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 428 6 2 6 4.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc([N+](=O)[O-])cc3)ccc2n1 10.1021/jm0002073
1691 2076 14 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
5311194 2076 14 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
CHEMBL357076 2076 14 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
10155966 188688 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 188688 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 90858 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 90858 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 178802 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 178802 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 90858 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 90858 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 172402 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 172402 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 5961 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 5961 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 95417 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 95417 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 91359 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 91359 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 138487 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 138487 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 125275 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 125275 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 152155 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 152155 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 98182 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 98182 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 98785 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 98785 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 183248 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 183248 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 5823 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 5823 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 211248 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 95984 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 95984 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 190175 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 190175 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 33778 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 33778 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 147899 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 147899 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 65811 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 65811 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 148499 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 148499 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 178052 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 178052 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 5972 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 5972 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 174689 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 174689 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 99129 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 99129 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 98162 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 98162 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 171829 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 171829 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 6108 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 6108 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 110516 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 110516 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 211389 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 146730 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 146730 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 64794 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 64794 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 114819 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 114819 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 114831 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 114831 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 114832 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 114832 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 185987 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 185987 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 178002 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 178002 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 102843 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 102843 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 91321 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 91321 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 91366 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 91366 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 113491 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 113491 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 35040 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 35040 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 90037 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 90037 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 162616 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 162616 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 176060 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 176060 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 176060 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 108258 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 108258 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 108258 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 108258 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 108258 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 108258 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 125276 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 125276 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 189041 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 189041 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 113391 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 113391 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 150824 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 150824 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 146446 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 146446 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 141880 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 141880 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 97446 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 97446 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 142724 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 142724 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 185726 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 185726 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 6280 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 6280 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 159366 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 159366 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 148576 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 148576 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 114833 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 114833 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 188576 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 188576 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 188576 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 188576 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 188576 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 188576 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 90029 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 90029 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 120463 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 120463 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 136476 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 136476 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 164103 19 None -19498 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 544 7 1 3 6.1 CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL421665 164103 19 None -19498 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 544 7 1 3 6.1 CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
46879627 6210 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 6210 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 175490 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 175490 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 173299 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 173299 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 86254 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 86254 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 63570 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 63570 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 97164 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 97164 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 77246 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 77246 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 77246 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 78266 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 78266 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 102911 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 102911 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 188762 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 188762 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 102849 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 102849 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 65373 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 65373 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 5891 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 5891 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 146358 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 146358 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 127656 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 127656 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 110108 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 110108 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 85272 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 85272 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 91274 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 91274 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 65930 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 65930 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 165728 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 165728 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 5795 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 5795 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 6144 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 6144 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 127660 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 127660 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 65975 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 65975 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 102917 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 102917 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 156861 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 156861 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 141557 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 141557 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 141557 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 141557 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 150465 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 150465 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 152727 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 152727 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 91145 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 91145 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 91145 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 91145 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 90196 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 90196 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 172578 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 172578 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 173981 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 173981 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 147901 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 147901 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 65832 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 65832 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 7386 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 7386 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 179424 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 179424 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 153304 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 153304 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 106781 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 106781 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 65376 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 65376 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 65240 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 65240 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 98833 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 98833 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 102910 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 102910 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 146592 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 146592 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 114811 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 114811 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 178550 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 178550 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 171165 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 171165 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 120887 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 120887 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 114822 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 114822 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 71494 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 71494 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 90696 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 90696 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 122797 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 122797 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 102914 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 102914 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 188752 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 188752 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 96193 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 96193 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 211326 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 153331 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 153331 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 90699 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 90699 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 211119 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 211586 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 212010 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 206381 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 206381 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 7437 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 7437 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 108131 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 108131 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 7448 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 7448 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 7449 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 7449 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 108044 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 108044 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 9108 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 9108 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 160757 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 160757 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 143745 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 143745 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 189174 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 189174 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 120890 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 120890 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 76303 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 76303 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 76304 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 76304 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 90031 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 90031 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 1286 39 None -43 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 1286 39 None -43 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 1286 39 None -43 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 1286 39 None -43 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 97220 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 97220 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 126771 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 126771 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 79312 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 79312 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 79312 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 106282 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 106282 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 168205 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 168205 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 114814 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 114814 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 114825 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 114825 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 171659 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 171659 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 139836 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 139836 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 78038 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 78038 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 102912 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 102912 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 2459 37 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 2459 37 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 2459 37 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 2459 37 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 62277 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 62277 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 5960 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 5960 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 193323 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 193323 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 65824 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 65824 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 158187 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 158187 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 178586 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 178586 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 63550 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 63550 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 177911 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 177911 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 76306 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 76306 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 102922 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 102922 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 114810 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 114810 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 102847 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 102847 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 5971 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 5971 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 89912 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 89912 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 90985 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 90985 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 4384 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 4384 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 170732 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 170732 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 95447 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 95447 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 138611 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 138611 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 79364 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 79364 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 120052 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 120052 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 120052 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 127666 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 127666 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 146285 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 146285 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 145903 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 145903 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 85258 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 85258 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 5797 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 5797 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 145605 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 145605 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 188616 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 188616 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 95991 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 95991 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 194460 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 194460 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 85300 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 85300 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 143457 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 143457 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 177934 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 177934 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 188617 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 188617 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 188854 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 188854 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 102842 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 102842 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 102869 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 102869 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 102873 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 102873 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 90195 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 90195 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 90197 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 90197 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 90457 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 90457 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 91465 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 91465 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 144985 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 144985 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 76308 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 76308 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 97551 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 97551 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 138505 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 138505 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 110515 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 110515 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 177115 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 177115 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 154470 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 154470 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 98198 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 98198 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 168074 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 168074 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 166148 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 166148 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 177965 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 177965 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 110514 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 110514 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 188656 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 188656 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 176221 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 176221 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 146766 0 None 14 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 335 3 1 3 3.2 CC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL392893 146766 0 None 14 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 335 3 1 3 3.2 CC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
46880116 7438 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 7438 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 95438 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 95438 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 138549 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 138549 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 188253 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 188253 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 188583 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 188583 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 211717 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 178606 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 178606 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 189486 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 189486 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 120058 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 120058 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 120058 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 65811 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 65811 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 159004 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 159004 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 76311 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 76311 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 187770 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 187770 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 95983 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 95983 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 66646 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 66646 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 162771 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 162771 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 90026 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 90026 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 211778 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 103048 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 103048 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 162812 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 162812 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 7649 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 7649 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 185989 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 185989 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 133058 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 133058 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 8860 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 8860 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 106781 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 106781 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 114836 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 114836 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 178003 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 178003 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 102850 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 102850 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 188516 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 188516 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 5965 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 5965 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 76305 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 76305 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 175502 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 175502 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 139972 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 139972 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 148131 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 148131 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 188267 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 188267 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 210929 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 211262 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 211674 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 129147 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 129147 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 127661 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 127661 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 58414 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 58414 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 5253 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 5253 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 85539 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 85539 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 136478 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 136478 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 151538 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 151538 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 66340 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 66340 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 114809 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 114809 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 106284 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 106284 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 7799 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 7799 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 120999 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 120999 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 102923 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 102923 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 86587 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 86587 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 114815 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 114815 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 179907 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 179907 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 120883 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 120883 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 152332 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 152332 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 120883 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 120883 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 151305 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 151305 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 110476 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 110476 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 110476 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 110476 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 65901 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 65901 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 110009 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 110009 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 120377 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 120377 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 85266 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 85266 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 114807 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 114807 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 7352 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 7352 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 127659 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 127659 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 78138 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 78138 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 143460 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 143460 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 65944 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 65944 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 64533 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 64533 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 102871 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 102871 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 91336 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 91336 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 148933 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 148933 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 149590 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 149590 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 9203 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 9203 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 30715 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 30715 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 109956 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 109956 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 64337 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 64337 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 168390 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 168390 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 31524 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc2c(N)n1 10.1021/jm0002073
CHEMBL140580 31524 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc2c(N)n1 10.1021/jm0002073
44395410 66558 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 405 6 1 2 5.8 OC1(c2ccc(Cl)cc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL186426 66558 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 405 6 1 2 5.8 OC1(c2ccc(Cl)cc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
68629836 152737 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 152737 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 90223 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 90223 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 188822 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 188822 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 153040 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 153040 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 139980 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 139980 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 64683 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 64683 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 177862 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 177862 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 99492 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 99492 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 64555 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 64555 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 114800 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 114800 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 114839 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 114839 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 210529 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 167296 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 167296 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 97500 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 97500 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 142375 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 142375 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 110465 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 110465 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 208850 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 127665 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 127665 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 165843 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 165843 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 138823 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 138823 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 85279 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 85279 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 142721 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 142721 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 114813 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 114813 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 188718 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 188718 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 102844 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 102844 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 89946 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 89946 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 90192 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 90192 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 90197 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 90197 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 90223 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 90223 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 144906 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 144906 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 165843 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 165843 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 127673 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 127673 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 178694 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 178694 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 90223 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 90223 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 168187 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 168187 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 95758 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 95758 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 57013 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 57013 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 57015 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 57015 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 57016 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 57016 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 178576 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 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 178576 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 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 188853 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 188853 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 120055 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 120055 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 120055 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 178586 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 178586 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 188653 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 188653 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 120050 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 120050 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 120050 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 77238 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 77238 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 57007 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 57007 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 77238 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 77238 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 87119 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 87119 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 175290 4 None 213 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4585935 175290 4 None 213 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
10475466 144452 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 144452 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 58434 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 58434 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 107415 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 107415 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 97294 0 None 812 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 340 2 1 2 3.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
CHEMBL271590 97294 0 None 812 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 340 2 1 2 3.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
46880114 7436 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 7436 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 57185 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 57185 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 155856 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 155856 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 157761 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 157761 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 146673 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 146673 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 178055 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 178055 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 188591 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 188591 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 65856 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 65856 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 90039 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 90039 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 139344 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 139344 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 102854 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 102854 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 145760 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 145760 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 77244 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 77244 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 77244 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 85514 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 85514 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 69975 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 69975 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 5932 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 5932 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 86176 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 86176 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 123483 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 123483 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 119765 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 119765 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 125367 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 125367 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 95384 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 95384 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 98721 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 98721 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 134690 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 134690 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 96851 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 96851 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 131968 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 131968 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 97511 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 97511 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 85294 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 85294 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 102867 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 102867 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 139838 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 139838 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 110894 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 110894 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 153655 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 153655 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 125281 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 125281 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 110463 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 110463 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 110463 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 110463 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 110463 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 110463 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 110463 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 110463 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 170495 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 170495 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 87317 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 87317 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 151305 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 151305 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 162645 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 162645 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 97942 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 97942 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 141556 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 141556 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 126873 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 126873 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 96556 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 96556 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 5890 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 5890 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 120893 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 120893 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 169278 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 169278 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 66721 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 66721 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 106279 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 106279 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 127658 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 127658 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 5821 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 5821 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 87774 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 87774 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 87630 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 87630 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 32886 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 32886 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 32886 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 168406 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 168406 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 65848 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 65848 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 30540 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 30540 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 96279 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 96279 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 110477 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 110477 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 143108 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 143108 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 102913 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 102913 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 102858 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 102858 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 139848 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 139848 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 165843 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 165843 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 178671 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 178671 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 120891 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 120891 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 6143 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 6143 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 5438 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 5438 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 86938 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 86938 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 143056 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 143056 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 180056 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 180056 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 62319 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 62319 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 5436 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 5436 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 7653 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 7653 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 178460 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 178460 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 145275 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 145275 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 147819 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 147819 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 172299 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 172299 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 102898 8 None 102 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 102898 8 None 102 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
44249047 102901 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 102901 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 85274 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 85274 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 144195 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 144195 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 114803 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 114803 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 188555 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 188555 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 5893 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 5893 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 90224 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 90224 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 90800 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 90800 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 144647 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 144647 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 65115 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 65115 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 203156 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 203156 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 77247 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 77247 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 188734 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 188734 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 7467 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 7467 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 90035 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387196 90035 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
44574790 188872 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 188872 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 77033 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 77033 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 83184 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 83184 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 142685 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 142685 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 178456 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 178456 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 113490 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 113490 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 120044 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 120044 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 120044 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 87504 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 87504 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 7478 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 7478 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 79884 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 79884 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 79884 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 138624 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 138624 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 76298 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 76298 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 99078 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 99078 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 127677 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 127677 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 77239 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 77239 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 77239 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 77239 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 106738 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 106738 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 138474 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 138474 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 191133 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 191133 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 125276 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 125276 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 171865 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 171865 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 170924 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 170924 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 95475 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 95475 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 95614 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 95614 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 148447 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 148447 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 114820 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 114820 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 114838 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 114838 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 116035 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 116035 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 1634 44 None -194 32 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 1634 44 None -194 32 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 1634 44 None -194 32 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 1634 44 None -194 32 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 1634 44 None -194 32 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 208899 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 66643 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 66643 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 123254 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 123254 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 153306 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 153306 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 78697 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 78697 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 97548 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 97548 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 86339 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 86339 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 186139 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 186139 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 127676 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 127676 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 65417 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 65417 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 77653 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 77653 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 77653 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 63129 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 63129 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 137853 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 137853 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 119900 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 119900 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 127667 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 127667 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 149555 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 149555 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 85270 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 85270 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 189159 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 189159 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 148855 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 148855 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 152737 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 152737 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 101266 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 101266 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 85301 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 85301 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 125868 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 125868 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 97252 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 97252 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 148152 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 148152 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 114801 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 114801 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 138535 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 138535 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 102872 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 102872 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 180059 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 180059 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 120888 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 120888 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 120889 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 120889 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 127678 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 127678 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 167897 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 167897 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 145605 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 145605 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 77303 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 77303 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 188994 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 188994 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 5156 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 5156 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 120894 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 120894 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 7651 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 7651 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 114817 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 114817 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 190597 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 190597 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 62315 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 62315 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 62316 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 62316 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 127670 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 127670 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 154436 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 154436 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 85310 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 85310 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 66538 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 66538 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 147676 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 147676 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 102907 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 102907 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 85293 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 85293 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 114804 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 114804 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 114828 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 114828 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 188864 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 188864 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 178026 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 178026 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 178210 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 178210 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 102848 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 102848 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 102863 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 102863 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 106808 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 106808 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 154439 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 154439 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 106808 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 106808 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 65811 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 65811 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 96982 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 96982 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 90698 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 90698 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 33006 4 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
5484063 33006 4 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL1418 33006 4 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
46879539 5420 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 5420 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 30833 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 30833 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 90033 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 90033 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 57011 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 57011 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 158430 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 158430 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 211391 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 178727 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 178727 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 99038 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 99038 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 91376 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 91376 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 91376 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 91376 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 65273 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 65273 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 62317 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 62317 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 171136 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 171136 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 59025 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 59025 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 128519 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 128519 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 65976 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 65976 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 90778 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 90778 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 127663 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 127663 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 85512 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 85512 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 139418 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 139418 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 87798 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 87798 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 114824 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 114824 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 7466 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 7466 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 120892 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 120892 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 145161 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 145161 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 65261 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 65261 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 132919 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 132919 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 127662 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 127662 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 146673 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 146673 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 64236 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 64236 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 127654 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 127654 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 211417 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 96580 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 96580 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 148604 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 148604 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 110011 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 110011 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 173728 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 173728 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 172104 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 172104 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 127653 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 127653 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 9235 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 9235 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 178646 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 178646 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 165801 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 165801 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 65377 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 65377 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 114823 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 114823 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 87322 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 87322 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 168258 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 168258 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 178053 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 178053 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 114835 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 114835 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 172299 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 172299 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 128520 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 128520 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 5144 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 5144 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 108692 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 108692 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 102905 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 102905 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 70278 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 70278 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 9011 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 9011 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 97021 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 97021 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 31010 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 31010 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 102920 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 102920 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 114805 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 114805 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 114818 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 114818 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 188875 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 188875 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 102845 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 102845 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 102862 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 102862 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 141137 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 141137 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 141137 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 5964 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 5964 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 58848 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 58848 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 96958 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 96958 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 99100 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 99100 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 177870 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 177870 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 77244 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 77244 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 77244 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 143964 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 143964 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 188715 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 188715 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 120038 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 120038 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 120038 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 124529 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 124529 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 4558 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 4558 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
11461888 4558 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 4558 2 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
10156821 177964 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 177964 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 90027 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 90027 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 5892 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 5892 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 95476 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 95476 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 114834 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 114834 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 193634 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 193634 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 206664 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 206664 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 79532 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 79532 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 124132 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 124132 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 109724 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 109724 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 106281 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 106281 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 85311 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 85311 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 102851 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 102851 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 144596 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 144596 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 5115 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 5115 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 147870 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 147870 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 114840 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 114840 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 97219 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 97219 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 5352 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 5352 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 102852 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 102852 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 110476 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 110476 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 140171 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 140171 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 150607 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 150607 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 110520 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 110520 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 32770 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 32770 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 32770 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 64127 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 64127 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 188576 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 188576 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 188576 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 188576 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 188576 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 188576 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 143056 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 143056 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 5125 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 5125 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 124996 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 124996 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 120057 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 120057 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 120057 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 100152 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 100152 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 5184 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 5184 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 102874 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 102874 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 120881 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 120881 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 96520 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 96520 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 120881 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 120881 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 120988 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 120988 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 188795 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 188795 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 177116 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 177116 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 71553 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 71553 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 2123 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
5311340 2123 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
CHEMBL140979 2123 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
1692 2123 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
5311340 2123 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
CHEMBL140979 2123 23 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
44574962 177938 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 177938 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 64937 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 64937 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 91345 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 91345 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 65370 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 65370 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 99069 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 99069 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 138595 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 138595 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 110517 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 110517 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 174230 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 174230 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 90036 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 90036 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 97501 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 97501 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 127657 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 127657 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 120885 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 120885 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 143976 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 143976 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 120885 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 120885 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 57012 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 57012 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 138415 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 138415 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 139022 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 139022 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 95517 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 95517 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 120045 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 120045 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 120045 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 65774 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 65774 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 85265 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 85265 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 114806 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 114806 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 164502 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 164502 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 137893 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 137893 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 120886 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 120886 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 79815 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 79815 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 79815 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 99045 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 99045 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 91288 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 91288 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 110154 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 110154 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 178647 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 178647 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 123167 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 123167 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 62323 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 62323 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 65608 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 65608 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 168249 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 168249 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 168249 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 178899 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 178899 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 87086 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 87086 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 34717 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 403 5 2 4 5.3 Nc1ccnc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc12 10.1021/jm0002073
CHEMBL143243 34717 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 403 5 2 4 5.3 Nc1ccnc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc12 10.1021/jm0002073
44252837 144277 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 144277 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 9255 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 9255 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 9255 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 9255 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 78603 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 78603 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 118724 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 118724 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 112370 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 112370 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 98869 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 98869 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 189119 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 189119 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 127669 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 127669 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 211443 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 144277 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 144277 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 102900 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 102900 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 102919 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 102919 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 85284 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 85284 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 161199 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 161199 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 102859 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 102859 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 166309 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 166309 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 168434 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 168434 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 125278 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 125278 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 83183 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 83183 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 77245 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 77245 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 120039 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 120039 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 120039 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 171571 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 171571 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 95363 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 95363 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 154212 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 154212 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 168970 0 None 38 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 168970 0 None 38 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
70682351 76310 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 76310 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 90030 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 90030 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 152759 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 152759 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 97497 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 97497 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 64513 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 64513 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 188800 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 188800 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 95466 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 95466 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 86920 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 86920 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 97560 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 97560 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 148938 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 148938 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 9072 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 9072 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 108207 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 108207 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 79544 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 79544 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 148604 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 148604 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 153306 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 153306 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 155649 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 155649 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 66886 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 66886 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 135492 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 135492 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 120880 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 120880 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 205923 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 205923 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 120880 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 120880 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 864 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 864 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 864 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 864 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 864 45 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
44413232 141003 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 141003 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 114826 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 114826 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 152505 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 152505 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 150632 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 150632 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 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
16131448 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1681 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1688 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
44361543 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
56947112 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
CHEMBL396460 2806 22 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1685 3866 0 None - 1 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15509719
23383556 178777 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 178777 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 189121 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 189121 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 178645 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 178645 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 178726 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 178726 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 178906 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 178906 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 179910 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 179910 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 189224 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 189224 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 178536 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 178536 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 188999 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 188999 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 178538 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 178538 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 180258 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 180258 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 189063 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 189063 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 178725 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 178725 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 189430 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 189430 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 179720 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 179720 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 188975 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 188975 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 189055 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 189055 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 178721 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 178721 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 178778 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 178778 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 90700 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 90700 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 178799 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 178799 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 188980 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 188980 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 178901 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 178901 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 179397 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 179397 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 179046 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 179046 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 188582 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 188582 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 214554 0 UNDEFINED -48977 6 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 215734 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 215736 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 215737 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 215738 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 187630 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 187630 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 178566 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 178566 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 189198 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 189198 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 178795 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 178795 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 189184 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 189184 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 179221 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 179221 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 179723 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 179723 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 189146 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 189146 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 174785 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 174785 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 90858 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 90858 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 178802 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 178802 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 190175 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 190175 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 174689 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 174689 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 189041 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 189041 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 91145 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 91145 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 179424 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 179424 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 189174 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 189174 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 177115 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 177115 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 176221 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 176221 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 188583 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 188583 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 189486 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 189486 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 187770 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 187770 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 188516 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 188516 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 179907 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 179907 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 178694 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 178694 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 215735 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 188653 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 188653 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 178671 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 178671 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 180056 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 180056 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 188555 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 188555 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 178456 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 178456 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 1634 44 UNDEFINED -194 32 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 1634 44 UNDEFINED -194 32 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 1634 44 UNDEFINED -194 32 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 1634 44 UNDEFINED -194 32 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 1634 44 UNDEFINED -194 32 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 189159 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 189159 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 180059 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 180059 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 188994 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 188994 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 1634 44 None -194 32 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 1634 44 None -194 32 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 1634 44 None -194 32 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 1634 44 None -194 32 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 1634 44 None -194 32 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 178727 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 178727 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 91376 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 91376 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 178646 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 178646 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 214227 0 None -5 8 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 2556 18 None -5 12 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 2556 18 None -5 12 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 2556 18 None -5 12 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 2556 18 None -5 12 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 2556 18 None -5 12 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 177116 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 177116 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 174230 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 174230 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 178647 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 178647 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 178899 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 178899 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 189119 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 189119 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 2439 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
24800108 2439 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
CHEMBL481512 2439 22 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
49843739 3611 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 3611 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 3611 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 3498 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 3498 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8870 505 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
91938095 505 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
CHEMBL3613442 505 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
8868 3491 27 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3491 27 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3491 27 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
11848225 864 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 864 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 864 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 864 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 864 45 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
11848225 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 864 45 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8868 3491 27 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3491 27 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3491 27 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
8868 3491 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 3491 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 3491 27 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
52914971 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
52914971 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
9462 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
9462 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
CHEMBL3304244 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
CHEMBL3304244 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
DB16048 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
DB16048 2375 28 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
16131448 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
16131448 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
16131448 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1681 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1681 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1681 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1688 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1688 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1688 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
44361543 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
44361543 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
44361543 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
56947112 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
56947112 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
56947112 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
CHEMBL396460 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL396460 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL396460 2806 22 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1694 3865 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
25081457 3865 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1682 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1682 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1682 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1682 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
6324645 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
6324645 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
6324645 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
6324645 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
CHEMBL384755 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL384755 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL384755 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL384755 2809 15 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
8865 3187 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24903280
1686 3024 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1686 3024 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15743186
50922685 725 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 725 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 2076 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
5311194 2076 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
CHEMBL357076 2076 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
1679 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1679 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
9963005 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL437723 266 21 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
132427684 506 0 None - 1 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 5 1 3 3.9 CNC(=O)CC1C(=O)N(c2c1cccc2)C1CCN(CC1)[C@@H]1CC[C@@H](CC1)C(C)C 29232769
9747 506 0 None - 1 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 5 1 3 3.9 CNC(=O)CC1C(=O)N(c2c1cccc2)C1CCN(CC1)[C@@H]1CC[C@@H](CC1)C(C)C 29232769
10047612 3473 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
10047612 3473 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1693 3473 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
1693 3473 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
CHEMBL559569 3473 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
CHEMBL559569 3473 14 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1684 3310 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
1684 3310 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
9844019 3310 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
9844019 3310 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
CHEMBL2088034 3310 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
CHEMBL2088034 3310 17 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
1680 267 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1680 267 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
15512229 3333 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 3333 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 3333 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 1027 20 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
7361 1027 20 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
CHEMBL201945 1027 20 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
1651 2679 22 None -19 9 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 2679 22 None -19 9 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 2679 22 None -19 9 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 2679 22 None -19 9 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 2679 22 None -19 9 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 2810 0 None - 1 Human 10.4 pKi None 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1696 3002 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
5311338 3002 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
1692 2123 23 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
5311340 2123 23 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
CHEMBL140979 2123 23 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
1695 2831 0 None - 1 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1679 266 21 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 266 21 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 266 21 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1680 267 0 None -2 2 Mouse 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1690 1606 0 None - 1 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
16131448 2806 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 2806 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 2806 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 2806 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 2806 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 2806 22 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
16143911 464 14 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
1689 464 14 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
CHEMBL505874 464 14 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863