Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
25208097 183330 3 None -1 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 183330 3 None -1 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
3917 3855 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1631926 207065 0 None - 1 Mouse 10.4 pEC50 = 10.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631926 207065 0 None - 1 Mouse 10.4 pEC50 = 10.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL264846 208877 0 None 12 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388462 161292 0 None 6 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None 6 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16131448 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1681 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1688 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
44361543 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
56947112 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
CHEMBL396460 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
16131448 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 2796 22 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44388461 159281 0 None 6 3 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None 6 3 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
24822630 97401 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL272215 97401 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL593215 97401 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
16131448 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 2796 22 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL409204 210994 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL261997 208769 6 None - 1 Human 9.8 pEC50 = 9.8 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL2372052 208419 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
16131448 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1681 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1688 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
44361543 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
56947112 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL396460 2796 22 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL265801 208908 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010221v
16131448 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1681 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1688 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44361543 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
56947112 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
CHEMBL396460 2796 22 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44388466 96041 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 96041 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL412537 211245 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1cccc(F)c1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL405648 210815 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL1627325 207058 0 None -8 8 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
CHEMBL427791 211624 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44388467 168828 0 None 4 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 168828 0 None 4 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
1682 2799 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
6324645 2799 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 2799 15 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL1631909 207059 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631909 207059 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
16131448 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1681 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1688 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
44361543 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
56947112 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
CHEMBL396460 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
12419 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 2429 22 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
16131448 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1681 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1688 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44361543 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
56947112 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL396460 2796 22 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44388462 161292 0 None -6 3 Mouse 9.4 pEC50 = 9.4 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None -6 3 Mouse 9.4 pEC50 = 9.4 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL263588 208824 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25208097 183330 3 None -1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481366 183330 3 None -1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
1682 2799 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
6324645 2799 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL384755 2799 15 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
3917 3855 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL429363 211768 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL1631923 207063 0 None - 1 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm101139f
CHEMBL1631923 207063 0 None - 1 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm101139f
3917 3855 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 3855 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 3855 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1162359 206765 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44388461 159281 0 None -6 3 Mouse 9.1 pEC50 = 9.1 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None -6 3 Mouse 9.1 pEC50 = 9.1 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414767 211396 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
1682 2799 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
6324645 2799 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 2799 15 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
16131448 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL507847 212775 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631926 207065 0 None - 1 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose in presence of compound 14 by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose in presence of compound 14 by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL428668 211707 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1F)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44388467 168828 0 None -4 2 Mouse 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 168828 0 None -4 2 Mouse 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
44388462 161292 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 161292 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16143911 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL511107 213807 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
1689 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 464 14 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1682 2799 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
6324645 2799 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 2799 15 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
44388461 159281 0 None -9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 159281 0 None -9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16131448 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL506825 212432 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
25207950 183204 0 None 120 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480426 183204 0 None 120 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
11956520 120041 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326228 120041 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545629 120041 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL556388 213948 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL559130 213956 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
25208095 190605 0 None 47 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL518950 190605 0 None 47 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL406097 210838 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Br)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
16131448 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
16131448 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1681 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1688 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
44361543 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
56947112 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 2796 22 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL1162358 206764 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
25208101 183331 0 None 181 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481367 183331 0 None 181 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
25208245 183352 0 None 478 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481547 183352 0 None 478 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
25208099 187776 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL501331 187776 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
11464846 77226 19 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 77226 19 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL5073561 212518 0 None 107 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL264846 208877 0 None -12 3 Guinea pig 8.7 pEC50 = 8.7 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
CHEMBL437915 211981 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm010092i
CHEMBL5070802 212463 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5080536 212909 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5093093 213621 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL504872 212404 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL262224 208779 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None Cc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
9927928 90024 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387199 90024 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL507653 212663 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44574791 177992 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467119 177992 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
71624265 90013 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387188 90013 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL442305 212152 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL504540 212399 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL526352 213896 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 2796 22 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 2799 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 2799 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 2799 15 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
76324308 102829 0 None 48 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084526 102829 0 None 48 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
16131448 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 2796 22 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 2799 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 2799 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 2799 15 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
10406239 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326224 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326226 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3545624 120036 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
56658044 65360 0 None -20 4 Human 7.0 pEC50 = 7.0 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834413 65360 0 None -20 4 Human 7.0 pEC50 = 7.0 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL5079432 212835 0 None -38 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)c1ccccc1 10.1021/acs.jmedchem.0c02062
CHEMBL442305 212152 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
9820782 142709 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389665 142709 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
9848990 188566 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL2368861 188566 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL511142 188566 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
134563650 169267 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439997 169267 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44426843 85286 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228964 85286 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
11164004 108051 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL320182 108051 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
10042904 206654 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL99738 206654 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL5078005 212746 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL525604 213871 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
10385808 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
8868 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 3478 27 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
49843555 56995 0 None 288 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650844 56995 0 None 288 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL438398 212012 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCC(CC)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL437192 211950 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCCC(CCC)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9842289 119964 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354291 119964 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL389521 210670 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
1679 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 266 21 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11956680 120034 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325961 120034 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3545622 120034 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
134563655 173636 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 173636 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
9803475 77227 22 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 77227 22 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL5087383 213307 0 None -7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
90655976 110507 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262549 110507 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
118718276 114802 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349260 114802 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
22562137 90023 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387198 90023 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
118718277 114803 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349261 114803 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
16131448 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL389521 210670 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
25208247 183353 0 None 676 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481548 183353 0 None 676 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
11848225 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 862 45 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
16131448 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL5086442 213246 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)cc1 10.1021/acs.jmedchem.0c02062
44430604 168195 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL437382 168195 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
53322001 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL1631924 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL265392 208889 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
46227961 13990 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198015 13990 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL593214 13990 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
44574705 178200 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468952 178200 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
71624269 90017 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387192 90017 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
129188462 175822 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4465668 175822 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4596017 175822 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10385808 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 65796 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
53322001 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL1631924 56119 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
42629117 177964 0 None 67 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466921 177964 0 None 67 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
122179052 120868 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581741 120868 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
76331525 102859 0 None 109 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084558 102859 0 None 109 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44430602 143910 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL390658 143910 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL556556 143910 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372051 208418 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372364 208418 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
81689704 120872 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581750 120872 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
16131448 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 2796 22 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
9848990 188566 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL2368861 188566 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL511142 188566 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL524873 213840 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
46227966 14049 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198704 14049 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611932 14049 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL389521 210670 0 None -11 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9954388 99065 1 None -4 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assay
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283480 99065 1 None -4 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assay
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL5081409 212965 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563496 173971 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4556227 173971 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
118718266 114792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349250 114792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL435511 211909 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
18782396 121157 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585388 121157 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586752 121157 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
44394284 65841 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184381 65841 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
44574588 177851 0 None 44 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466067 177851 0 None 44 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574585 178042 0 None 56 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL467488 178042 0 None 56 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
11451023 106725 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL316699 106725 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL268394 208995 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL396972 210744 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44394324 65809 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184234 65809 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
129188443 168959 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 168959 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
122179061 120879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581757 120879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44394283 65817 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184260 65817 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10155966 188678 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL511920 188678 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
44394375 123154 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL362160 123154 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
10139672 125354 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL364844 125354 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
53325608 56998 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650847 56998 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
44456216 154849 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL403588 154849 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL398224 210762 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCC(CC)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5093399 213640 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
3655995 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL320874 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
3655995 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
CHEMBL320874 108245 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
134563699 175492 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4591048 175492 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44456187 95184 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL257921 95184 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
76320665 102850 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084549 102850 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL5070616 212460 0 None 20 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44456141 94897 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL256687 94897 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44430602 143910 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL390658 143910 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL556556 143910 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5081993 212999 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
9905428 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL505824 212416 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL264846 208877 0 None -17 3 Mouse 8.6 pEC50 = 8.6 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25207948 183203 0 None 18 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480425 183203 0 None 18 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL5074745 212549 0 None 15 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02062
CHEMBL499157 212310 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL5081578 212972 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44248674 102912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084677 102912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45271534 193576 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551111 193576 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45268153 194450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL561115 194450 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45269032 194500 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
CHEMBL561373 194500 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
44247589 102832 0 None 37 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084529 102832 0 None 37 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46227963 14046 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198701 14046 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611929 14046 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
9905428 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 4328 12 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
9925137 120038 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326222 120038 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3545626 120038 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
44394419 65864 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184451 65864 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
101886205 121160 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585402 121160 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586792 121160 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
1684 3298 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 3298 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 3298 17 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
16131448 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
86279209 110502 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262544 110502 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL405645 210812 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
44394381 66631 0 None 25 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL186822 66631 0 None 25 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL507269 212505 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL384866 210582 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
9844540 85278 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228911 85278 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
10274330 66325 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL185415 66325 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
9863568 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
53316968 56992 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650841 56992 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
44456296 97258 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL271478 97258 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44456298 168227 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL437601 168227 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL2372051 208418 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372364 208418 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
122179060 120878 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581756 120878 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
122179064 120882 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581762 120882 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL405645 210812 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL427954 211638 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(N)=O 10.1016/j.bmcl.2006.04.086
54756990 65358 0 None -2754 3 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834411 65358 0 None -2754 3 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
16131448 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1681 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1688 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
44361543 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
56947112 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 2796 22 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL5085090 213165 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563704 176050 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4451073 176050 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4597933 176050 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
16131448 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 2796 22 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL424934 211569 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
CHEMBL415781 211442 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL262928 208798 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
10109899 85269 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228857 85269 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL5094655 213719 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
9803475 77227 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
CHEMBL2088036 77227 22 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
10042904 162759 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL418980 162759 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL266667 208938 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
10042904 90012 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387187 90012 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL5094439 213709 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
25235412 102830 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084527 102830 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
25235412 114818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349276 114818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44430588 86391 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL232245 86391 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL541911 86391 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44456220 154888 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL403807 154888 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
22558157 110505 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262547 110505 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
16665918 79324 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211722 79324 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
134578342 172482 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
CHEMBL4519453 172482 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
44181744 102885 8 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 102885 8 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
11461888 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
11461888 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 4543 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL405948 210830 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
9863568 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL3809510 210518 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL394588 210720 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCCC(CCC)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL442113 212149 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL1631922 207062 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC1=O 10.1021/jm101139f
CHEMBL1631922 207062 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC1=O 10.1021/jm101139f
25208249 183373 0 None 1202 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481707 183373 0 None 1202 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL555757 213945 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 213894 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL558807 213955 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44551464 14048 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198703 14048 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611931 14048 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL5079758 212856 0 None 151 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL1631921 207061 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm101139f
1641 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
3829 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
5497186 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL567175 2678 6 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL406718 210860 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
16131448 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 2796 22 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL455289 212239 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631925 207064 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631925 207064 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL5081139 212944 0 None 12 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
71624387 90020 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387195 90020 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
10134217 65929 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184698 65929 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL269029 209020 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL269029 209020 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL265544 208898 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44456185 166057 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL428076 166057 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
5268 3586 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
53 3586 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL300555 3586 34 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL505873 212418 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
10137876 124516 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364398 124516 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
9863568 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 141545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
122179056 120874 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581752 120874 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
10110916 65915 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184646 65915 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44394487 65100 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182967 65100 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
134563466 170716 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4460695 170716 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574789 177963 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
CHEMBL466919 177963 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
16131448 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 2796 22 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None