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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 | |
| CHEMBL1380104 | 28960 | None | 4 | Human | Binding | Ki | = | 3280.00 | 5.48 | - | 1 | Displacement of (S)-N-(1-(2-[3H]-4-methoxyphenyl)propan-2-yl)-2-(2,3-dimethyl-7-oxothieno[2,3-d]pyridazin-6(7H)-yl)acetamide from human GPR139 expressed in CHO-TRex membranes incubated for 20 mins by scintillation counting assay | ChEMBL | 338.1 | 6 | 1 | 6 | 1.16 | COc1ccc(CCNC(=O)Cn2nnc3ccccc3c2=O)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.1c00820 | |
| CHEMBL4740228 | 179525 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 2 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 363.1 | 4 | 1 | 6 | 2.12 | CC(C(=O)N[C@@H](C)c1ccc(Cl)c(F)c1)n1nc2cccnn2c1=O | - | |
| CHEMBL4740228 | 179525 | None | 0 | Rat | Binding | EC50 | = | 10.00 | 8.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 363.1 | 4 | 1 | 6 | 2.12 | CC(C(=O)N[C@@H](C)c1ccc(Cl)c(F)c1)n1nc2cccnn2c1=O | - | |
| CHEMBL4740228 | 179525 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 363.1 | 4 | 1 | 6 | 2.12 | CC(C(=O)N[C@@H](C)c1ccc(Cl)c(F)c1)n1nc2cccnn2c1=O | - | |
| CHEMBL4740491 | 179550 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 411.1 | 6 | 1 | 8 | 1.68 | COc1cnc2nn(CC(=O)N[C@@H](C)c3ccc(OC(F)(F)F)cc3)c(=O)n2c1 | - | |
| CHEMBL4740519 | 179553 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 434.1 | 5 | 1 | 8 | 1.40 | C[C@H](NC(=O)Cn1nc2cc(N3CCOCC3)cnn2c1=O)c1ccc(Cl)c(F)c1 | - | |
| CHEMBL4741467 | 179639 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 377.1 | 4 | 1 | 6 | 2.18 | Cc1cc(C)n2c(=O)n(CC(=O)N[C@@H](C)c3ccc(Cl)c(F)c3)nc2n1 | - | |
| CHEMBL4742901 | 179741 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 363.1 | 4 | 1 | 6 | 1.87 | Cc1ccn2c(=O)n(CC(=O)N[C@@H](C)c3ccc(Cl)c(F)c3)nc2n1 | - | |
| CHEMBL4742949 | 179743 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 378.1 | 5 | 1 | 6 | 2.17 | COc1ccn2c(=O)n(CC(=O)N[C@@H](C)c3ccc(Cl)c(F)c3)nc2c1 | - | |
| CHEMBL4743612 | 179793 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 348.1 | 4 | 1 | 5 | 2.17 | C[C@H](NC(=O)Cn1nc2ccccn2c1=O)c1ccc(Cl)c(F)c1 | - | |
| CHEMBL4743662 | 179799 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 324.2 | 4 | 1 | 5 | 1.99 | Cc1ccc([C@H](C)NC(=O)Cn2nc3cc(C)ccn3c2=O)cc1 | - | |
| CHEMBL4743938 | 179816 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 324.2 | 4 | 1 | 5 | 2.24 | Cc1ccc([C@H](C)NC(=O)C(C)n2nc3ccccn3c2=O)cc1 | - | |
| CHEMBL4743938 | 179816 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 324.2 | 4 | 1 | 5 | 2.24 | Cc1ccc([C@H](C)NC(=O)C(C)n2nc3ccccn3c2=O)cc1 | - | |
| CHEMBL4744340 | 179864 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 479.2 | 6 | 2 | 8 | 2.23 | C[C@H](NC(=O)Cn1nc2cc(N3CCC[C@@H](O)C3)ccn2c1=O)c1ccc(OC(F)(F)F)cc1 | - | |
| CHEMBL4744737 | 179893 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 2 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 363.1 | 4 | 1 | 6 | 1.87 | Cc1ccnn2c(=O)n(CC(=O)N[C@@H](C)c3ccc(Cl)c(F)c3)nc12 | - | |
| CHEMBL4744737 | 179893 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 363.1 | 4 | 1 | 6 | 1.87 | Cc1ccnn2c(=O)n(CC(=O)N[C@@H](C)c3ccc(Cl)c(F)c3)nc12 | - | |
| CHEMBL4744927 | 179916 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 364.0 | 4 | 1 | 5 | 2.68 | C[C@H](NC(=O)Cn1nc2ccccn2c1=O)c1ccc(Cl)c(Cl)c1 | - | |
| CHEMBL4744927 | 179916 | None | 0 | Rat | Binding | EC50 | = | 1.00 | 9.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 364.0 | 4 | 1 | 5 | 2.68 | C[C@H](NC(=O)Cn1nc2ccccn2c1=O)c1ccc(Cl)c(Cl)c1 | - | |
| CHEMBL4744984 | 179920 | None | 0 | Rat | Binding | EC50 | = | 10.00 | 8.00 | - | 2 | Agonist activity at rat GPR139 expressed in CHO-K1 cells assessed as increase in calcium flux by calcium 5 dye based FLIPR assay | ChEMBL | 337.2 | 5 | 1 | 6 | 1.65 | C[C@H](NC(=O)Cn1nc2cccnn2c1=O)c1ccc(C2CC2)cc1 | - | |
| CHEMBL4745096 | 179941 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 2 | Agonist activity at human GPR139 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay | ChEMBL | 399.1 | 5 | 1 | 7 | 1.81 | C[C@H](NC(=O)Cn1nc2cccnn2c1=O)c1ccc(OC(F)(F)F)c(F)c1 | - | |
Showing 1 to 20 of 273 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 | |
| CHEMBL1310918 | 20937 | None | 11 | Human | Functional | EC50 | = | 1303.00 | 5.88 | - | 1 | Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assay | ChEMBL | 308.1 | 5 | 1 | 5 | 1.15 | O=C(Cn1nnc2ccccc2c1=O)NCCc1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.1c00820 | |
| CHEMBL1380104 | 28960 | None | 4 | Human | Functional | EC50 | = | 46.00 | 7.34 | - | 1 | Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assay | ChEMBL | 338.1 | 6 | 1 | 6 | 1.16 | COc1ccc(CCNC(=O)Cn2nnc3ccccc3c2=O)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.1c00820 | |
| CHEMBL1460960 | 38115 | None | 4 | Human | Functional | EC50 | = | 66.00 | 7.18 | - | 1 | Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assay | ChEMBL | 334.1 | 3 | 1 | 5 | 1.99 | O=C(Cn1nnc2ccccc2c1=O)NC1CCCc2ccccc21 | https://dx.doi.org/10.1021/acs.jmedchem.1c00820 | |
| CHEMBL1546963 | 47659 | None | 5 | Human | Functional | EC50 | = | 293.00 | 6.53 | - | 1 | Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assay | ChEMBL | 328.1 | 4 | 1 | 5 | 1.76 | O=C(Cn1nnc2ccccc2c1=O)NCc1ccc(Cl)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.1c00820 | |
| CHEMBL3633714 | 124181 | None | 0 | Human | Functional | EC50 | = | 66.00 | 7.18 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 326.2 | 6 | 2 | 3 | 2.69 | COc1cccc(C(=O)N[C@@H](C)C(=O)N[C@@H](C)c2ccccc2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633715 | 124182 | None | 0 | Human | Functional | EC50 | = | 440.00 | 6.36 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 326.2 | 6 | 2 | 3 | 2.69 | COc1cccc(C(=O)N[C@H](C)C(=O)N[C@@H](C)c2ccccc2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633716 | 124183 | None | 0 | Human | Functional | EC50 | = | 283.00 | 6.55 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 342.2 | 7 | 3 | 4 | 1.66 | COc1cccc(C(=O)N[C@@H](CO)C(=O)N[C@@H](C)c2ccccc2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633717 | 124184 | None | 0 | Human | Functional | EC50 | = | 10000.00 | 5.00 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 402.2 | 8 | 2 | 3 | 3.91 | COc1cccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C)c2ccccc2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633718 | 124185 | None | 0 | Human | Functional | EC50 | = | 162.00 | 6.79 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 282.1 | 5 | 2 | 2 | 2.29 | C[C@H](NC(=O)CNC(=O)c1ccccc1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633719 | 124186 | None | 0 | Human | Functional | EC50 | = | 150.00 | 6.82 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 316.1 | 5 | 2 | 2 | 2.95 | C[C@H](NC(=O)CNC(=O)c1ccccc1Cl)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633721 | 124187 | None | 1 | Human | Functional | EC50 | = | 118.00 | 6.93 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 316.1 | 5 | 2 | 2 | 2.95 | C[C@H](NC(=O)CNC(=O)c1ccc(Cl)cc1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633878 | 124191 | None | 0 | Human | Functional | EC50 | = | 24.00 | 7.62 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 296.2 | 5 | 2 | 2 | 2.60 | Cc1cccc(C(=O)NCC(=O)N[C@@H](C)c2ccccc2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633879 | 124192 | None | 0 | Human | Functional | EC50 | = | 59.00 | 7.23 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 307.1 | 5 | 2 | 3 | 2.17 | C[C@H](NC(=O)CNC(=O)c1cccc(C#N)c1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633880 | 124193 | None | 0 | Human | Functional | EC50 | = | 54.00 | 7.27 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 300.1 | 5 | 2 | 2 | 2.43 | C[C@H](NC(=O)CNC(=O)c1cccc(F)c1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633881 | 124194 | None | 0 | Human | Functional | EC50 | = | 33.00 | 7.48 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 312.1 | 6 | 2 | 3 | 2.30 | COc1cccc(C(=O)NCC(=O)N[C@@H](C)c2ccccc2)c1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633882 | 124195 | None | 0 | Human | Functional | EC50 | = | 52.00 | 7.28 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 350.1 | 5 | 2 | 2 | 3.31 | C[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633883 | 124196 | None | 0 | Human | Functional | EC50 | = | 46.00 | 7.34 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 366.1 | 6 | 2 | 3 | 3.19 | C[C@H](NC(=O)CNC(=O)c1cccc(OC(F)(F)F)c1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633884 | 124197 | None | 0 | Human | Functional | EC50 | = | 52.00 | 7.28 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 350.1 | 5 | 2 | 2 | 3.60 | C[C@H](NC(=O)CNC(=O)c1cccc(Cl)c1Cl)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633885 | 124198 | None | 1 | Human | Functional | EC50 | = | 193.00 | 6.71 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 350.1 | 5 | 2 | 2 | 3.60 | C[C@H](NC(=O)CNC(=O)c1ccc(Cl)c(Cl)c1)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
| CHEMBL3633886 | 124199 | None | 0 | Human | Functional | EC50 | = | 40.00 | 7.40 | - | 1 | Agonist activity at human GPR139 receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | ChEMBL | 350.1 | 5 | 2 | 2 | 3.60 | C[C@H](NC(=O)CNC(=O)c1cc(Cl)ccc1Cl)c1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.5b00247 | |
Showing 1 to 20 of 369 entries