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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 | |
| CHEMBL3727412 | 135367 | None | 0 | Human | Binding | Ki | = | 134.00 | 6.87 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 534.2 | 7 | 1 | 6 | 4.66 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)CCc1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3727434 | 135372 | None | 0 | Human | Binding | Ki | = | 6.00 | 8.22 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 554.2 | 5 | 1 | 7 | 4.38 | C[C@H](Nc1nc2c(c(=O)n1N1CCCC1)CN(C(=O)c1ccc(C#N)cc1F)CC2)c1ccc(C(F)(F)F)cc1 | - | |
| CHEMBL3727443 | 135375 | None | 0 | Human | Binding | Ki | = | 10.00 | 8.00 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 492.1 | 5 | 1 | 7 | 4.06 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C)s1)CC2 | - | |
| CHEMBL3727469 | 135382 | None | 0 | Human | Binding | Ki | = | 6.00 | 8.22 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 527.2 | 7 | 1 | 8 | 3.33 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)COc1ccc(C#N)cc1)CC2 | - | |
| CHEMBL3727905 | 135454 | None | 0 | Human | Binding | Ki | = | 17.00 | 7.77 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 543.2 | 6 | 1 | 8 | 4.69 | CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3cccnc3s1)CC2 | - | |
| CHEMBL3728036 | 135471 | None | 0 | Human | Binding | Ki | = | 2.00 | 8.70 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 537.2 | 6 | 1 | 6 | 4.67 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2 | - | |
| CHEMBL3728036 | 135471 | None | 0 | Human | Binding | Ki | = | 2.00 | 8.70 | - | 1 | Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times. | ChEMBL | 537.2 | 6 | 1 | 6 | 4.67 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2 | - | |
| CHEMBL3728107 | 135484 | None | 0 | Human | Binding | Ki | = | 26.00 | 7.58 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 561.2 | 7 | 1 | 7 | 5.31 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(-c3cnco3)cc1)CC2 | - | |
| CHEMBL3728107 | 135484 | None | 0 | Human | Binding | Ki | = | 26.00 | 7.58 | - | 1 | Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times. | ChEMBL | 561.2 | 7 | 1 | 7 | 5.31 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(-c3cnco3)cc1)CC2 | - | |
| CHEMBL3728239 | 135509 | None | 0 | Human | Binding | Ki | = | 25.00 | 7.60 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 520.1 | 6 | 1 | 6 | 4.74 | CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3728315 | 135522 | None | 0 | Human | Binding | Ki | = | 9.00 | 8.05 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 529.1 | 5 | 1 | 8 | 4.30 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3cccnc3s1)CC2 | - | |
| CHEMBL3728379 | 135534 | None | 0 | Human | Binding | Ki | = | 6.00 | 8.22 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 498.2 | 6 | 1 | 6 | 4.33 | C=Cc1ccc(C(=O)N2CCc3nc(N[C@@H](C)c4ccc(C(F)(F)F)cc4)n(OC)c(=O)c3C2)cc1 | - | |
| CHEMBL3728379 | 135534 | None | 0 | Human | Binding | Ki | = | 6.00 | 8.22 | - | 1 | Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times. | ChEMBL | 498.2 | 6 | 1 | 6 | 4.33 | C=Cc1ccc(C(=O)N2CCc3nc(N[C@@H](C)c4ccc(C(F)(F)F)cc4)n(OC)c(=O)c3C2)cc1 | - | |
| CHEMBL3728578 | 135573 | None | 0 | Human | Binding | Ki | = | 121.00 | 6.92 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 554.1 | 7 | 1 | 6 | 5.30 | COn1c(NC(CCC(F)(F)F)c2ccc(Cl)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3728578 | 135573 | None | 0 | Human | Binding | Ki | = | 121.00 | 6.92 | - | 1 | Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times. | ChEMBL | 554.1 | 7 | 1 | 6 | 5.30 | COn1c(NC(CCC(F)(F)F)c2ccc(Cl)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3728601 | 135576 | None | 0 | Human | Binding | Ki | = | 18.00 | 7.75 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 536.1 | 6 | 1 | 7 | 4.35 | COc1cc(Cl)ccc1C(=O)N1CCc2nc(N[C@@H](C)c3ccc(C(F)(F)F)cc3)n(OC)c(=O)c2C1 | - | |
| CHEMBL3728776 | 135603 | None | 0 | Human | Binding | Ki | = | 15.00 | 7.82 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 530.2 | 5 | 1 | 7 | 3.11 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3c(s1)=CCCC=3)CC2 | - | |
| CHEMBL3728824 | 135612 | None | 0 | Human | Binding | Ki | = | 24.00 | 7.62 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 545.2 | 5 | 1 | 6 | 5.21 | CC#CCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc3ccccc3n1)CC2 | - | |
| CHEMBL3728824 | 135612 | None | 0 | Human | Binding | Ki | = | 24.00 | 7.62 | - | 1 | Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times. | ChEMBL | 545.2 | 5 | 1 | 6 | 5.21 | CC#CCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc3ccccc3n1)CC2 | - | |
| CHEMBL3729024 | 135641 | None | 0 | Human | Binding | Ki | = | 20.00 | 7.70 | - | 1 | Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | ChEMBL | 558.2 | 6 | 1 | 9 | 4.15 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc(-c3cccs3)n(C)n1)CC2 | - | |
Showing 1 to 20 of 190 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 | |
| CHEMBL3727412 | 135367 | None | 0 | Human | Functional | IC50 | = | 3896.00 | 5.41 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 534.2 | 7 | 1 | 6 | 4.66 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)CCc1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3727434 | 135372 | None | 0 | Human | Functional | IC50 | = | 298.00 | 6.53 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 554.2 | 5 | 1 | 7 | 4.38 | C[C@H](Nc1nc2c(c(=O)n1N1CCCC1)CN(C(=O)c1ccc(C#N)cc1F)CC2)c1ccc(C(F)(F)F)cc1 | - | |
| CHEMBL3727443 | 135375 | None | 0 | Human | Functional | IC50 | = | 1128.00 | 5.95 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 492.1 | 5 | 1 | 7 | 4.06 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C)s1)CC2 | - | |
| CHEMBL3727905 | 135454 | None | 0 | Human | Functional | IC50 | = | 1684.00 | 5.77 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 543.2 | 6 | 1 | 8 | 4.69 | CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3cccnc3s1)CC2 | - | |
| CHEMBL3728036 | 135471 | None | 0 | Human | Functional | IC50 | = | 68.00 | 7.17 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 537.2 | 6 | 1 | 6 | 4.67 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2 | - | |
| CHEMBL3728036 | 135471 | None | 0 | Human | Functional | IC50 | = | 68.00 | 7.17 | - | 1 | Intracellular Calcium Mobilization Assay: HEK293 cells expressing human GPR10 were maintained in Dulbecco's Modified Eagles' medium supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin and 20 mM HEPES at 37° C. in a 5% CO2 incubator. GPR10-expressing HEK293 cells were placed in poly-D-lysine coated 96-well culture plates and cultured for 18-24 hr before the test at a density of 3×104 cells/well. The cells were incubated with 2.5 nM Fluo-8 for 1 hr at room temperature in Recording Buffer containing 1% bovine serum albumin, 0.01% pluronic F-127 and 20 mM HEPES, Hanks Balanced Buffered Saline, pH 7.4. The cells were incubated with test compounds for 15 min at room temperature, and then PrRP (the final concentration, 1 nM) was added into the medium. The changes in intracellular calcium-dependent fluorescence were monitored using a fluorescence imaging plate reader (FDSS3000, Hamamatsu Photonics K.K.). Fluo-8 fluorescence was measured with excitation at 490 nm and emission at 520 nm. | ChEMBL | 537.2 | 6 | 1 | 6 | 4.67 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2 | - | |
| CHEMBL3728239 | 135509 | None | 0 | Human | Functional | IC50 | = | 3710.00 | 5.43 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 520.1 | 6 | 1 | 6 | 4.74 | CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3728824 | 135612 | None | 0 | Human | Functional | IC50 | = | 3350.00 | 5.47 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 545.2 | 5 | 1 | 6 | 5.21 | CC#CCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc3ccccc3n1)CC2 | - | |
| CHEMBL3728824 | 135612 | None | 0 | Human | Functional | IC50 | = | 3350.00 | 5.47 | - | 1 | Intracellular Calcium Mobilization Assay: HEK293 cells expressing human GPR10 were maintained in Dulbecco's Modified Eagles' medium supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin and 20 mM HEPES at 37° C. in a 5% CO2 incubator. GPR10-expressing HEK293 cells were placed in poly-D-lysine coated 96-well culture plates and cultured for 18-24 hr before the test at a density of 3×104 cells/well. The cells were incubated with 2.5 nM Fluo-8 for 1 hr at room temperature in Recording Buffer containing 1% bovine serum albumin, 0.01% pluronic F-127 and 20 mM HEPES, Hanks Balanced Buffered Saline, pH 7.4. The cells were incubated with test compounds for 15 min at room temperature, and then PrRP (the final concentration, 1 nM) was added into the medium. The changes in intracellular calcium-dependent fluorescence were monitored using a fluorescence imaging plate reader (FDSS3000, Hamamatsu Photonics K.K.). Fluo-8 fluorescence was measured with excitation at 490 nm and emission at 520 nm. | ChEMBL | 545.2 | 5 | 1 | 6 | 5.21 | CC#CCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc3ccccc3n1)CC2 | - | |
| CHEMBL3729087 | 135652 | None | 0 | Human | Functional | IC50 | = | 227.00 | 6.64 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 529.2 | 6 | 1 | 7 | 4.09 | CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2 | - | |
| CHEMBL3729094 | 135654 | None | 0 | Human | Functional | IC50 | = | 4494.00 | 5.35 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 500.1 | 6 | 1 | 6 | 4.62 | COn1c(NC(c2ccc(Cl)cc2)C(C)C)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3729094 | 135654 | None | 0 | Human | Functional | IC50 | = | 4494.00 | 5.35 | - | 1 | Intracellular Calcium Mobilization Assay: HEK293 cells expressing human GPR10 were maintained in Dulbecco's Modified Eagles' medium supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin and 20 mM HEPES at 37° C. in a 5% CO2 incubator. GPR10-expressing HEK293 cells were placed in poly-D-lysine coated 96-well culture plates and cultured for 18-24 hr before the test at a density of 3×104 cells/well. The cells were incubated with 2.5 nM Fluo-8 for 1 hr at room temperature in Recording Buffer containing 1% bovine serum albumin, 0.01% pluronic F-127 and 20 mM HEPES, Hanks Balanced Buffered Saline, pH 7.4. The cells were incubated with test compounds for 15 min at room temperature, and then PrRP (the final concentration, 1 nM) was added into the medium. The changes in intracellular calcium-dependent fluorescence were monitored using a fluorescence imaging plate reader (FDSS3000, Hamamatsu Photonics K.K.). Fluo-8 fluorescence was measured with excitation at 490 nm and emission at 520 nm. | ChEMBL | 500.1 | 6 | 1 | 6 | 4.62 | COn1c(NC(c2ccc(Cl)cc2)C(C)C)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3729152 | 135662 | None | 0 | Human | Functional | IC50 | = | 686.00 | 6.16 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 556.2 | 6 | 1 | 7 | 4.59 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(OC(F)(F)F)cc1)CC2 | - | |
| CHEMBL3729222 | 135673 | None | 0 | Human | Functional | IC50 | = | 1183.00 | 5.93 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 502.1 | 7 | 1 | 7 | 3.75 | COn1c(N[C@H](C)c2ccc(Cl)cc2)nc2c(c1=O)CN(C(=O)COc1ccc(Cl)cc1)CC2 | - | |
| CHEMBL3729468 | 135710 | None | 0 | Human | Functional | IC50 | = | 1031.00 | 5.99 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 500.2 | 5 | 1 | 6 | 4.31 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C)c(C)c1)CC2 | - | |
| CHEMBL3729902 | 135786 | None | 0 | Human | Functional | IC50 | = | 62.00 | 7.21 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 519.2 | 6 | 1 | 6 | 4.53 | C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1)CC2 | - | |
| CHEMBL3730005 | 135801 | None | 0 | Human | Functional | IC50 | = | 3600.00 | 5.44 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 515.1 | 7 | 1 | 7 | 3.88 | C[C@H](Nc1nc2c(c(=O)n1N(C)C)CN(C(=O)COc1ccc(Cl)cc1)CC2)c1ccc(Cl)cc1 | - | |
| CHEMBL3730415 | 135869 | None | 0 | Human | Functional | IC50 | = | 824.00 | 6.08 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 546.1 | 5 | 1 | 7 | 5.09 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3cc(Cl)ccc3o1)CC2 | - | |
| CHEMBL3731175 | 136002 | None | 0 | Human | Functional | IC50 | = | 648.00 | 6.19 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 536.2 | 5 | 1 | 7 | 4.24 | C[C@H](Nc1nc2c(c(=O)n1N1CCCC1)CN(C(=O)c1ccc(C#N)cc1)CC2)c1ccc(C(F)(F)F)cc1 | - | |
| CHEMBL3731182 | 136004 | None | 0 | Human | Functional | IC50 | = | 286.00 | 6.54 | - | 1 | Antagonist activity against human GPR10 receptor expressed in HEK293 cells assessed as inhibition of PrRP-induced intracellular calcium mobilization pre-incubated for 15 mins before PrRP addition by Fluo-8 dye based fluorescence imaging plate reader method | ChEMBL | 523.2 | 5 | 1 | 7 | 4.24 | COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cnc3ccccc3c1)CC2 | - | |
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