| Tclin | Adenosine receptor A2a |
This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily, which is subdivided into classes and subtypes. The receptors are seven-pass transmembrane proteins that respond to extracellular cues and activate intracellular signal transduction pathways. This protein, an adenosine receptor of A2A subtype, uses adenosine as the preferred endogenous agonist and preferentially interacts with the G(s) and G(olf) family of G proteins to increase intracellular cAMP levels. It plays an important role in many biological functions, such as cardiac rhythm and circulation, cerebral and renal blood flow, immune function, pain regulation, and sleep. It has been implicated in pathophysiological conditions such as inflammatory diseases and neurodegenerative disorders. Alternative splicing results in multiple transcript variants. A read-through transcript composed of the upstream SPECC1L (sperm antigen with calponin homology and coiled-coil domains 1-like) and ADORA2A (adenosine A2a receptor) gene sequence has been identified, but it is thought to be non-coding. [provided by RefSeq, Jun 2013]
Comments
Property Summary
| Ligand Count | 1,516 |
| NCBI Gene PubMed Count | 307 |
| PubMed Score | 954.12 |
| PubTator Score | 555.51 |
| Disease | Target Count |
|---|---|
| Schizophrenia | 1160 |
| Adverse reaction to drug | 61 |
| Drug allergy | 36 |
| Hyperactive behavior | 91 |
| Mood Disorders | 184 |
| Rheumatoid arthritis | 1191 |
| Disease | Target Count | Z-score | Confidence |
|---|---|---|---|
| Huntington's disease | 76 | 3.905 | 2.0 |
| Vascular disease | 319 | 3.755 | 1.9 |
| Lesch-Nyhan syndrome | 12 | 3.097 | 1.5 |
theophylline
pKi 9.22
caffeine
pKi 5.61
regadenoson
pEC50 5.89
adenosine
pEC50 6.15
choline theophyllinate
pKi 9.22
bufylline
pKi 9.22
istradefylline
pKi 8.66
CHEMBL3125711
pKi 7.00
CHEMBL349716
pKi 7.00
CHEMBL456125
pKi 7.00
CHEMBL199898
pKi 7.00
CHEMBL165560
pKi 7.00
CHEMBL1170135
pKi 7.00
CHEMBL488152
pKi 7.00
CHEMBL1950659
pKi 7.00
CHEMBL331372
pKd 7.00
CHEMBL3133067
pKi 7.00
CHEMBL589251
pKi 7.00
CHEMBL3754353
pKi 7.00
CHEMBL139182
pKi 7.00
CHEMBL166424
pKi 7.00
CHEMBL520031
pKi 7.00
CHEMBL167343
pKi 7.00
CHEMBL194696
pKi 7.00
CHEMBL3797433
pKi 7.00
CHEMBL118923
pKi 7.00
CHEMBL355761
pKi 7.00
MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAIPFAITISTGF 1 - 70 CAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTRAKGIIAICWVLSFAIGLTPM 71 - 140 LGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYFNFFACVLVPLLLMLGVYLRIFLAARRQLKQ 141 - 210 MESQPLPGERARSTLQKEVHAAKSLAIIVGLFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTN 211 - 280 SVVNPFIYAYRIREFRQTFRKIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGS 281 - 350 APHPERRPNGYALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS 351 - 412 //
