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 | |
| CHEMBL3092287 | 103959 | None | 0 | Human | Binding | IC50 | = | 200.00 | 6.70 | - | 2 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 411.1 | 8 | 1 | 4 | 3.78 | COc1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(C(=O)O)cc2)cc1 | - | |
| CHEMBL3890262 | 142551 | None | 0 | Human | Binding | IC50 | = | 20.00 | 7.70 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 380.2 | 5 | 1 | 7 | 2.09 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(Cc3ccccc3N)C2=O)cn1 | - | |
| CHEMBL3890303 | 142556 | None | 0 | Human | Binding | IC50 | = | 190.00 | 6.72 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 424.2 | 6 | 0 | 8 | 2.69 | COc1ccc(CN2C(=O)N(c3cnn(Cc4c(C)noc4C)c3)C(=O)C2(C)C)nc1 | - | |
| CHEMBL3890306 | 142557 | None | 0 | Human | Binding | IC50 | = | 610.00 | 6.21 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 356.1 | 6 | 1 | 7 | 2.81 | COc1cccc(C(=O)Nc2cnn(Cc3c(C)noc3C)c2)c1OC | - | |
| CHEMBL3890651 | 142604 | None | 0 | Human | Binding | IC50 | = | 700.00 | 6.16 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 370.1 | 5 | 1 | 8 | 2.53 | COc1cc(C(=O)Nc2cnn(Cc3c(C)noc3C)c2)cc2c1OCO2 | - | |
| CHEMBL3890731 | 142612 | None | 0 | Human | Binding | IC50 | = | 830.00 | 6.08 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 338.2 | 7 | 1 | 5 | 3.50 | Cc1noc(C)c1Cn1cc(NC(=O)CCCc2ccccc2)cn1 | - | |
| CHEMBL3891080 | 142656 | None | 0 | Human | Binding | IC50 | = | 130.00 | 6.89 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 425.2 | 6 | 2 | 8 | 1.96 | Cc1noc(C)c1Cn1cc(N2C(=O)N(Cc3cccc(O)c3)C(C)(CO)C2=O)cn1 | - | |
| CHEMBL3891877 | 142750 | None | 0 | Human | Binding | IC50 | = | 400.00 | 6.40 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 354.1 | 4 | 1 | 7 | 2.56 | Cc1noc(C)c1Cn1cc(NC(=O)c2ccc3c(c2)OCCO3)cn1 | - | |
| CHEMBL3892375 | 142818 | None | 0 | Human | Binding | IC50 | = | 250.00 | 6.60 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 437.2 | 7 | 0 | 7 | 3.33 | COc1cccc(CCN2C(=O)N(c3cnn(Cc4c(C)noc4C)c3)C(=O)C2(C)C)c1 | - | |
| CHEMBL3892490 | 142836 | None | 0 | Human | Binding | IC50 | = | 40.00 | 7.40 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 418.2 | 5 | 0 | 7 | 3.15 | Cc1noc(C)c1Cn1cc(N2C(=O)N(Cc3ccc(C#N)cc3)C(C)(C)C2=O)cn1 | - | |
| CHEMBL3892490 | 142836 | None | 0 | Human | Binding | IC50 | = | 50.00 | 7.30 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 418.2 | 5 | 0 | 7 | 3.15 | Cc1noc(C)c1Cn1cc(N2C(=O)N(Cc3ccc(C#N)cc3)C(C)(C)C2=O)cn1 | - | |
| CHEMBL3892633 | 142856 | None | 0 | Human | Binding | IC50 | = | 2640.00 | 5.58 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 470.2 | 8 | 0 | 6 | 4.44 | Cc1noc(C)c1Cn1cc(N2CN(Cc3ccccc3)CN(CCc3ccccc3)C2=O)cn1 | - | |
| CHEMBL3892982 | 142902 | None | 0 | Human | Binding | IC50 | = | 100.00 | 7.00 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 388.1 | 4 | 1 | 7 | 3.21 | Cc1noc(C)c1Cn1cc(NC(=O)c2cc(Cl)c3c(c2)OCCO3)cn1 | - | |
| CHEMBL3893359 | 142952 | None | 0 | Human | Binding | IC50 | = | 600.00 | 6.22 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 354.1 | 4 | 1 | 7 | 2.56 | Cc1noc(C)c1Cn1cc(NC(=O)c2cccc3c2OCCO3)cn1 | - | |
| CHEMBL3893402 | 142955 | None | 0 | Human | Binding | IC50 | = | 70.00 | 7.16 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 435.2 | 5 | 1 | 7 | 3.52 | Cc1noc(C)c1Cn1cc(N2C(=O)N(Cc3cccc(O)c3)C3(CCCC3)C2=O)cn1 | - | |
| CHEMBL3894018 | 143024 | None | 0 | Human | Binding | IC50 | = | 1350.00 | 5.87 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 285.1 | 4 | 2 | 5 | 2.12 | Cc1noc(C)c1Cn1cc(NC(=O)c2cc[nH]c2)cn1 | - | |
| CHEMBL3894331 | 143055 | None | 0 | Human | Binding | IC50 | = | 700.00 | 6.16 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 322.1 | 5 | 1 | 5 | 3.19 | Cc1noc(C)c1Cn1cc(NC(=O)/C=C/c2ccccc2)cn1 | - | |
| CHEMBL3894430 | 143073 | None | 0 | Human | Binding | IC50 | = | 100.00 | 7.00 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 407.2 | 5 | 0 | 6 | 3.59 | Cc1ccccc1CN1C(=O)N(c2cnn(Cc3c(C)noc3C)c2)C(=O)C1(C)C | - | |
| CHEMBL3894433 | 143074 | None | 0 | Human | Binding | IC50 | = | 800.00 | 6.10 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 365.1 | 5 | 1 | 7 | 3.49 | CCc1nc2cc(C(=O)Nc3cnn(Cc4c(C)noc4C)c3)ccc2o1 | - | |
| CHEMBL3894555 | 143080 | None | 0 | Human | Binding | IC50 | = | 400.00 | 6.40 | - | 1 | Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels. | ChEMBL | 427.1 | 6 | 0 | 7 | 2.24 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(Cc3ccccc3[S+](C)[O-])C2=O)cn1 | - | |
Showing 1 to 20 of 314 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 | |
| andrographolide | 416 | None | 0 | Human | Functional | pEC50 | = | - | 3.96 | -8 | 3 | Unclassified | Guide to Pharmacology | 350.2 | 3 | 3 | 5 | 1.96 | C=C1CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)CO)[C@@H]1C/C=C1/C(=O)OC[C@H]1O | https://pubmed.ncbi.nlm.nih.gov/32330040 | |
| CHEMBL3890731 | 142612 | None | 0 | Human | Functional | IC50 | = | 800.00 | 6.10 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 338.2 | 7 | 1 | 5 | 3.50 | Cc1noc(C)c1Cn1cc(NC(=O)CCCc2ccccc2)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3891080 | 142656 | None | 0 | Human | Functional | IC50 | = | 100.00 | 7.00 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 425.2 | 6 | 2 | 8 | 1.96 | Cc1noc(C)c1Cn1cc(N2C(=O)N(Cc3cccc(O)c3)C(C)(CO)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3891877 | 142750 | None | 0 | Human | Functional | IC50 | = | 400.00 | 6.40 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 354.1 | 4 | 1 | 7 | 2.56 | Cc1noc(C)c1Cn1cc(NC(=O)c2ccc3c(c2)OCCO3)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3896824 | 143358 | None | 0 | Human | Functional | IC50 | = | 100.00 | 7.00 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 381.1 | 5 | 1 | 7 | 2.21 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(Cc3ccccc3O)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3898835 | 143600 | None | 0 | Human | Functional | IC50 | = | 200.00 | 6.70 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 322.1 | 3 | 0 | 6 | 2.34 | Cc1noc(C)c1Cn1cc(N2C(=O)c3ccccc3C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3899757 | 143713 | None | 0 | Human | Functional | IC50 | = | 700.00 | 6.16 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 326.1 | 5 | 1 | 6 | 2.80 | COc1ccc(C(=O)Nc2cnn(Cc3c(C)noc3C)c2)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3899833 | 143725 | None | 0 | Human | Functional | IC50 | = | 500.00 | 6.30 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 390.1 | 5 | 0 | 7 | 2.38 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(Cc3ccccc3C#N)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3901756 | 143960 | None | 0 | Human | Functional | IC50 | = | 300.00 | 6.52 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 371.2 | 5 | 0 | 6 | 2.88 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(CC3CCCCC3)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3902340 | 144030 | None | 0 | Human | Functional | IC50 | = | 100.00 | 7.00 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 422.2 | 6 | 1 | 7 | 1.86 | CNC(=O)c1cccc(CN2CC(=O)N(c3cnn(Cc4c(C)noc4C)c3)C2=O)c1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3902844 | 144094 | None | 0 | Human | Functional | IC50 | = | 4600.00 | 5.34 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 297.1 | 4 | 1 | 6 | 2.18 | Cc1noc(C)c1Cn1cc(NC(=O)c2ccncc2)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3908324 | 144756 | None | 0 | Human | Functional | IC50 | = | 800.00 | 6.10 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 310.1 | 5 | 1 | 5 | 2.72 | Cc1noc(C)c1Cn1cc(NC(=O)Cc2ccccc2)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3908801 | 144812 | None | 0 | Human | Functional | IC50 | = | 1900.00 | 5.72 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 326.1 | 5 | 1 | 6 | 2.80 | COc1ccccc1C(=O)Nc1cnn(Cc2c(C)noc2C)c1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3910649 | 145057 | None | 0 | Human | Functional | IC50 | = | 1000.00 | 6.00 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 359.2 | 5 | 0 | 7 | 1.48 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(CC3CCCO3)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3911209 | 145127 | None | 0 | Human | Functional | IC50 | = | 2300.00 | 5.64 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 297.1 | 4 | 1 | 6 | 2.18 | Cc1noc(C)c1Cn1cc(NC(=O)c2ccccn2)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3911225 | 145129 | None | 0 | Human | Functional | IC50 | = | 9000.00 | 5.05 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 308.1 | 3 | 0 | 5 | 2.70 | Cc1noc(C)c1Cn1cc(N2Cc3ccccc3C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3911861 | 145206 | None | 0 | Human | Functional | IC50 | = | 18000.00 | 4.75 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 314.1 | 4 | 1 | 7 | 1.83 | Cc1cc(C(=O)Nc2cnn(Cc3c(C)noc3C)c2)n(C)n1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3912134 | 145238 | None | 0 | Human | Functional | IC50 | = | 1000.00 | 6.00 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 366.1 | 5 | 0 | 7 | 1.90 | Cc1noc(C)c1Cn1cc(N2C(=O)CN(Cc3ccccn3)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3915586 | 145698 | None | 0 | Human | Functional | IC50 | = | 40.00 | 7.40 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 411.2 | 6 | 2 | 8 | 1.57 | Cc1noc(C)c1Cn1cc(N2C(=O)[C@H](CO)N(Cc3cccc(O)c3)C2=O)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
| CHEMBL3916540 | 145828 | None | 0 | Human | Functional | IC50 | = | 1100.00 | 5.96 | - | 1 | Antagonist activity at recombinant human TAS2R8 stably expressed in cells co-expressing Galpha16gust44 assessed as inhibition of andrographolide-induced intracellular calcium level measured for 100 secs by fluo-4 dye based FLIPR assay | ChEMBL | 297.1 | 4 | 1 | 6 | 2.18 | Cc1noc(C)c1Cn1cc(NC(=O)c2cccnc2)cn1 | https://dx.doi.org/10.1021/acs.jmedchem.0c00388 | |
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