Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | adenosine A1 receptor | Starlite/ChEMBL | References |
Homo sapiens | adenosine A3 receptor | Starlite/ChEMBL | References |
Homo sapiens | adenosine A2a receptor | Starlite/ChEMBL | References |
Homo sapiens | adenosine A2b 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 |
---|---|---|---|---|
Schistosoma mansoni | alpha(13)fucosyltransferase | 0.0095 | 1 | 1 |
Brugia malayi | alpha1,3-fucosyltransferase homologue | 0.0095 | 1 | 0.5 |
Schistosoma mansoni | alpha(13)fucosyltransferase | 0.0095 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0095 | 1 | 0.5 |
Schistosoma mansoni | alpha(13)fucosyltransferase | 0.0095 | 1 | 1 |
Loa Loa (eye worm) | fucosyl transferase | 0.0095 | 1 | 0.5 |
Schistosoma mansoni | alpha(13)fucosyltransferase | 0.0095 | 1 | 1 |
Schistosoma mansoni | alpha(13)fucosyltransferase | 0.0095 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 8.2 nM | Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 4.4-15.2 | ChEMBL. | 11831890 |
IC50 (functional) | = 8.2 nM | Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 4.4-15.2 | ChEMBL. | 11831890 |
Ki (binding) | = 6.04 | Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins | ChEMBL. | 21163647 |
Ki (binding) | = 9.041 | Binding affinity to human adenosine A3 receptor | ChEMBL. | No reference |
Ki (binding) | = 0.91 nM | Displacement of [3H]-MRE3008-F20 binding at human Adenosine A3 receptor expressed in HEK cells; range 0.82-1.01 | ChEMBL. | 11831890 |
Ki (binding) | = 0.91 nM | Binding affinity for human adenosine A3 receptor | ChEMBL. | 15634009 |
Ki (binding) | = 0.91 nM | Displacement of [3H]-MRE3008-F20 binding at human Adenosine A3 receptor expressed in HEK cells; range 0.82-1.01 | ChEMBL. | 11831890 |
Ki (binding) | = 0.91 nM | Binding affinity for human adenosine A3 receptor | ChEMBL. | 15634009 |
Ki (binding) | = 0.91 nM | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells | ChEMBL. | 19501513 |
Ki (binding) | = 101 nM | Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK-293 cells; range 89-116 | ChEMBL. | 11831890 |
Ki (binding) | = 101 nM | Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK-293 cells; range 89-116 | ChEMBL. | 11831890 |
Ki (binding) | = 200 nM | Displacement of [3H]-SCH-58,261 from human Adenosine A2A receptor expressed in HEK-293 cells; range 174-230 | ChEMBL. | 11831890 |
Ki (binding) | = 200 nM | Displacement of [3H]-SCH-58,261 from human Adenosine A2A receptor expressed in HEK-293 cells; range 174-230 | ChEMBL. | 11831890 |
Ki (binding) | = 200 nM | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | ChEMBL. | 19501513 |
Ki (binding) | = 400 nM | Displacement of [3H]-DPCPX from human Adenosine A1 receptor expressed in CHO cells; range 332-479 | ChEMBL. | 11831890 |
Ki (binding) | = 400 nM | Displacement of [3H]-DPCPX from human Adenosine A1 receptor expressed in CHO cells; range 332-479 | ChEMBL. | 11831890 |
pKi (binding) | = -2.3 nM | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | ChEMBL. | 19501513 |
pKi (binding) | = 0.04 nM | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells | ChEMBL. | 19501513 |
Ratio (binding) | = 111 | Selectivity ratio of the compound (h2B/hA3) | ChEMBL. | 11831890 |
Ratio (binding) | = 220 | Selectivity ratio of the compound (h2A/hA3) | ChEMBL. | 11831890 |
Ratio (binding) | = 440 | 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.