Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | adenosine A2a receptor | Starlite/ChEMBL | References |
Homo sapiens | adenosine A2b receptor | Starlite/ChEMBL | References |
Homo sapiens | adenosine A3 receptor | Starlite/ChEMBL | References |
Homo sapiens | adenosine A1 receptor | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | hypothetical protein | adenosine A1 receptor | 326 aa | 305 aa | 21.0 % |
Brugia malayi | follicle stimulating hormone receptor | adenosine A2a receptor | 412 aa | 336 aa | 22.3 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Armadillo/beta-catenin-like repeat family protein | 0.0094 | 0.0031 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0229 | 0.6851 | 1 |
Loa Loa (eye worm) | HMP-2 protein | 0.0094 | 0.0031 | 0.5 |
Echinococcus multilocularis | beta catenin | 0.0094 | 0.0031 | 0.5 |
Onchocerca volvulus | Cirhin homolog | 0.0093 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 2.4 nM | Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor; range 1.2-4.9 | ChEMBL. | 11831890 |
IC50 (functional) | = 2.4 nM | Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor; range 1.2-4.9 | ChEMBL. | 11831890 |
Ki (binding) | = 6.54 | Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins | ChEMBL. | 21163647 |
Ki (binding) | = 9.538 | Binding affinity to human adenosine A3 receptor | ChEMBL. | No reference |
Ki (binding) | = 0.29 nM | Displacement of [3H]-MRE3008-F20 from human Adenosine A3 receptor expressed in HEK cells; range 0.23-0.36 | ChEMBL. | 11831890 |
Ki (binding) | = 0.29 nM | Binding affinity for human adenosine A3 receptor | ChEMBL. | 15634009 |
Ki (binding) | = 0.29 nM | Displacement of [3H]-MRE3008-F20 from human Adenosine A3 receptor expressed in HEK cells; range 0.23-0.36 | ChEMBL. | 11831890 |
Ki (binding) | = 0.29 nM | Binding affinity for human adenosine A3 receptor | ChEMBL. | 15634009 |
Ki (binding) | = 0.29 nM | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells | ChEMBL. | 19501513 |
Ki (binding) | = 128 nM | Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK-293 cells; range 115-143 | ChEMBL. | 11831890 |
Ki (binding) | = 128 nM | Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK-293 cells; range 115-143 | ChEMBL. | 11831890 |
Ki (binding) | = 180 nM | Displacement of [3H]-SCH-58,261 from human Adenosine A2A receptor expressed in HEK-293 cells; range 162-200 | ChEMBL. | 11831890 |
Ki (binding) | = 180 nM | Displacement of [3H]-SCH-58,261 from human Adenosine A2A receptor expressed in HEK-293 cells; range 162-200 | ChEMBL. | 11831890 |
Ki (binding) | = 180 nM | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | ChEMBL. | 19501513 |
Ki (binding) | = 430 nM | Displacement of [3H]-DPCPX from human Adenosine A1 receptor expressed in CHO cells; range 351-526 | ChEMBL. | 11831890 |
Ki (binding) | = 430 nM | Displacement of [3H]-DPCPX from human Adenosine A1 receptor expressed in CHO cells; range 351-526 | ChEMBL. | 11831890 |
pKi (binding) | = -2.26 nM | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | ChEMBL. | 19501513 |
pKi (binding) | = 0.54 nM | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells | ChEMBL. | 19501513 |
Ratio (binding) | = 441 | Selectivity ratio of the compound (h2B/hA3) | ChEMBL. | 11831890 |
Ratio (binding) | = 621 | Selectivity ratio of the compound (h2A/hA3) | ChEMBL. | 11831890 |
Ratio (binding) | = 1483 | Selectivity ratio of the compound (hA1/hA3) | ChEMBL. | 11831890 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
4 literature references were collected for this gene.