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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
[Ala31,Aib32]NPY | 335 | None | 0 | Rat | Binding | pKi | None | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12890716 | |
[D-Trp32]NPY | 1500 | None | 0 | Human | Binding | pKi | None | - | 8.10 | -1 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8824284 | |
[D-Trp32]NPY | 1500 | None | 0 | Rat | Binding | pKi | None | - | 8.20 | 1 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8824284 | |
[Leu31,Pro34]NPY (pig) | 2303 | None | 0 | Human | Binding | pKi | None | - | 9.10 | 1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8824284 | |
[Leu31,Pro34]NPY (pig) | 2303 | None | 0 | Rat | Binding | pKi | None | - | 8.95 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8824284 | |
[Leu31,Pro34]NPY (pig) | 2303 | None | 0 | Rat | Binding | pKi | None | - | 8.95 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12890716 | |
[Leu31,Pro34]PYY (human) | 2304 | None | 0 | Human | Binding | pKi | = | - | 8.80 | -25 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8824284 | |
[Leu31,Pro34]PYY (human) | 2304 | None | 0 | Rat | Binding | pKi | None | - | 8.70 | -31 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8824284 | |
[PP1-17,Ala31,Aib32]NPY (human) | 3155 | None | 0 | Human | Binding | pKi | None | - | 8.80 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12890716 | |
ATC0175 | 511 | None | 14 | Human | Binding | IC50 | = | 2700.00 | 5.57 | - | 7 | Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells | ChEMBL | 425.2 | 5 | 2 | 5 | 4.13 | CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.05.121 | |
BENEXTRAMINE | 67670 | None | 3 | Human | Binding | Ki | = | 5000.00 | 5.30 | -2 | 2 | Binding affinity to NPY5 receptor | ChEMBL | 590.4 | 27 | 4 | 8 | 6.26 | COc1ccccc1CNCCCCCCNCCSSCCNCCCCCCNCc1ccccc1OC | https://dx.doi.org/10.1016/j.bmcl.2011.06.124 | |
BIBO3304 | 630 | None | 18 | Rat | Binding | IC50 | = | 21000.00 | 4.68 | - | 4 | Radioligand binding assay (rat NPY5R, CHO cells) | ChEMBL | 529.3 | 13 | 6 | 4 | 1.84 | NC(=O)NCc1ccc(CNC(=O)[C@@H](CCCN=C(N)N)NC(=O)C(c2ccccc2)c2ccccc2)cc1 | https://dx.doi.org/10.6019/CHEMBL5463723 | |
BIBO3304 | 218915 | 125I-hPP | 0 | Rat | Binding | pKi | = | 1000.00 | 6.00 | - | 1 | - | PDSP KiDatabase | 643.3 | 13 | 7 | 5 | 2.48 | NC(=O)NCc1ccc(CNC(=O)C(CCCN=C(N)N)NC(=O)C(c2ccccc2)c2ccccc2)cc1.O=C(O)C(F)(F)F | - | |
BIIE0246 | 218722 | 125I-hPP | 0 | Rat | Binding | pKi | = | 1000.00 | 6.00 | -131 | 3 | - | PDSP KiDatabase | 895.4 | 16 | 5 | 11 | 3.29 | NC(N)=NCCCC(NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O | - | |
CGP 71683A | 899 | None | 11 | Human | Binding | IC50 | = | 1.30 | 8.89 | - | 8 | Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY | ChEMBL | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.03.052 | |
CGP 71683A | 899 | None | 11 | Human | Binding | IC50 | = | 2.90 | 8.54 | - | 8 | Compound was tested for human Neuropeptide Y receptor type 5 | ChEMBL | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | https://dx.doi.org/10.1016/s0960-894x(00)00177-3 | |
CGP 71683A | 899 | None | 11 | Human | Binding | IC50 | = | 2.90 | 8.54 | - | 8 | Human Neuropeptide Y5 receptor binding affinity | ChEMBL | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2003.11.070 | |
CGP 71683A | 899 | None | 11 | Rat | Binding | pKi | None | - | 9.50 | 2 | 8 | Unclassified | Guide to Pharmacology | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/12890716 | |
CGP 71683A | 899 | 125I-hPP | 11 | Rat | Binding | pKi | = | 1.10 | 8.96 | 2 | 8 | - | PDSP KiDatabase | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | - | |
CGP 71683A | 899 | None | 11 | Rat | Binding | IC50 | = | 1.40 | 8.85 | 2 | 8 | Compound was tested for rat Neuropeptide Y receptor type 5 | ChEMBL | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | https://dx.doi.org/10.1016/s0960-894x(00)00177-3 |
Showing 1 to 20 of 1,413 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
[Ala31,Aib32]NPY (pig) | 336 | None | 0 | Human | Functional | pIC50 | = | - | 8.20 | 1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12069595 | |
[Ala31,Aib32]NPY (pig) | 336 | None | 0 | Rat | Functional | pIC50 | = | - | 8.20 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12069595 | |
CGP 71683A | 899 | None | 11 | Human | Functional | IC50 | = | 2.90 | 8.54 | -1 | 8 | Compound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cells | ChEMBL | 475.2 | 7 | 3 | 6 | 4.56 | Nc1nc(NCC2CCC(CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 | https://dx.doi.org/10.1016/s0960-894x(00)00177-3 | |
CHEMBL1208795 | 14974 | None | 0 | Human | Functional | Ki | = | 50.12 | 7.30 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 377.1 | 5 | 1 | 6 | 3.03 | O=C(c1ccncc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1208996 | 14988 | None | 0 | Human | Functional | Ki | = | 2511.89 | 5.60 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 314.1 | 4 | 1 | 5 | 2.34 | CC(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209049 | 14994 | None | 0 | Human | Functional | Ki | = | 2.51 | 8.60 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 342.2 | 5 | 1 | 5 | 2.98 | CC(C)C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209050 | 14995 | None | 0 | Human | Functional | Ki | = | 12.59 | 7.90 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 376.1 | 5 | 1 | 5 | 3.63 | O=C(c1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209051 | 14996 | None | 0 | Human | Functional | Ki | = | 2.51 | 8.60 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 376.1 | 5 | 1 | 5 | 3.63 | O=C(c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209052 | 14997 | None | 0 | Human | Functional | Ki | = | 1.00 | 9.00 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 394.1 | 5 | 1 | 5 | 3.77 | O=C(c1cccc(F)c1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209053 | 14998 | None | 0 | Human | Functional | Ki | = | 1.58 | 8.80 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 412.1 | 5 | 1 | 5 | 3.91 | O=C(c1cc(F)cc(F)c1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209100 | 15003 | None | 0 | Human | Functional | Ki | = | 5.01 | 8.30 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 377.1 | 5 | 1 | 6 | 3.03 | O=C(c1cccnc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209101 | 15004 | None | 0 | Human | Functional | Ki | = | 1.00 | 9.00 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 390.2 | 6 | 1 | 5 | 3.56 | O=C(Cc1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209102 | 15005 | None | 0 | Human | Functional | Ki | = | 1.00 | 9.00 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 390.2 | 6 | 1 | 5 | 3.56 | O=C(Cc1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209159 | 15015 | None | 0 | Human | Functional | Ki | = | 0.40 | 9.40 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 404.2 | 6 | 1 | 5 | 4.13 | CC(C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209160 | 15016 | None | 0 | Human | Functional | Ki | = | 0.79 | 9.10 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 416.2 | 6 | 1 | 5 | 4.05 | O=C(N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)C1(c2ccccc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209161 | 15017 | None | 0 | Human | Functional | Ki | = | 6.31 | 8.20 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 404.2 | 7 | 1 | 5 | 3.95 | O=C(CCc1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209162 | 15018 | None | 0 | Human | Functional | Ki | = | 0.63 | 9.20 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 404.2 | 7 | 1 | 5 | 3.95 | O=C(CCc1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209215 | 15028 | None | 0 | Human | Functional | Ki | = | 5.01 | 8.30 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 432.2 | 7 | 1 | 5 | 4.76 | CC(C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)C(C)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209216 | 15029 | None | 0 | Human | Functional | Ki | = | 0.79 | 9.10 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 416.2 | 6 | 1 | 5 | 4.13 | O=C([C@H]1C[C@@H]1c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 | |
CHEMBL1209217 | 15030 | None | 0 | Human | Functional | Ki | = | 7.94 | 8.10 | - | 1 | Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay | ChEMBL | 370.1 | 5 | 1 | 6 | 2.36 | O=C(C1CCOC1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 | https://dx.doi.org/10.1016/j.bmcl.2010.06.140 |
Showing 1 to 20 of 265 entries