For Research Use Only Highly sensitive GPCR evaluation service.
Tanso Biosciences: GPCR functional profiling services
GPCRs are known to be extremely important therapeutic target molecules in many diseases. Almost 40% of currently approved medical products display clinical effects by acting against GPCRs. Although more than 300 GPCRs, excluding sensory receptors, have been annotated in humans, only a limited number of GPCRs have been used in medical drugs. The progress of new drug discovery for over 200 GPCRs is impeded by lack of assay methodology to evaluate candidate drug compounds and difficulty of pharmacological analysis.
Tanso Biosciences has developed a highly sensitive functional profiling platform for all human GPCRs, including GPCRs whose activity cannot be assessed by currently available methods, by combining proprietary reporter cell lines and Gα-proteins. We also offer GPCR Custom Profiling Services, which can be utilized for a variety of purposes including discovery of on-target molecules (ligands), validation of off-target effects on other receptors, and screening and optimization for specific GPCRs.
Advantages
- High sensitivity, high signal-to-background ratio (Fig. 2) achieved with Tanso Biosciences proprietary assay method (Fig. 1)
- Not only agonist and inverse agonist, but antagonist, PAM, and NAM can be assessed for ligand known GPCRs
- A total of 313 human GPCRs (excluding sensory receptors) are covered.
- High sensitivity assessment for G12/13 and Gi/o coreceptors, which are difficult to evaluate by conventional activity assays.
- Compatibility with all Gα proteins allows assaying orphan receptors (agonist, inverse agonist mode)
- Cost effective and short turn around time (Results will be delivered in 2 - 3 weeks after sample receipt).
Principle
Fig. 1 Principle of GPCR Assay
A GPCR activated by its ligand can activate multiple cellular signal transduction pathways through associated G proteins. In Tanso Biosciences' GPCR assay platform, we utilize proprietary reporter cell lines. In these cells, signals that have diverged into downstream cellular signal transduction pathways will be re-converged, and then amplified by accumulation effect. In this novel technology, sample-specific stimulation against target GPCR can be assessed with high sensitivity, using reporter Luciferase activity as an indicator.
Representative Results
Fig. 2 Comparison between conventional assay (left: J Biol Chem. 1995;270:12846-50.) and Tanso Biosciences custom assay (right).
Right: The agonist response for AGTR1 was assessed using Tanso Biosciences' assay. The results showed almost 100 fold higher sensitivity compared to conventional method, and achieved high S/B ratio.
List of Targets
| Symbol | Nomenclature | Family | |
|---|---|---|---|
| 1 | HTR1A | 5-HT1A receptor | 5-Hydroxytryptamine receptors |
| 2 | HTR1B | 5-HT1B receptor | 5-Hydroxytryptamine receptors |
| 3 | HTR1D | 5-HT1D receptor | 5-Hydroxytryptamine receptors |
| 4 | HTR1E | 5-ht1e receptor | 5-Hydroxytryptamine receptors |
| 5 | HTR1F | 5-HT1F receptor | 5-Hydroxytryptamine receptors |
| 6 | HTR2A | 5-HT2A receptor | 5-Hydroxytryptamine receptors |
| 7 | HTR2B | 5-HT2B receptor | 5-Hydroxytryptamine receptors |
| 8 | HTR2C | 5-HT2C receptor | 5-Hydroxytryptamine receptors |
| 9 | HTR4 | 5-HT4 receptor | 5-Hydroxytryptamine receptors |
| 10 | HTR5A | 5-HT5A receptor | 5-Hydroxytryptamine receptors |
| 11 | HTR6 | 5-HT6 receptor | 5-Hydroxytryptamine receptors |
| 12 | HTR7 | 5-HT7 receptor | 5-Hydroxytryptamine receptors |
| 13 | CHRM1 | M1 receptor | Acetylcholine receptors (muscarinic) |
| 14 | CHRM2 | M2 receptor | Acetylcholine receptors (muscarinic) |
| 15 | CHRM3 | M3 receptor | Acetylcholine receptors (muscarinic) |
| 16 | CHRM4 | M4 receptor | Acetylcholine receptors (muscarinic) |
| 17 | CHRM5 | M5 receptor | Acetylcholine receptors (muscarinic) |
| 18 | ADORA1 | A1 receptor | Adenosine receptors |
| 19 | ADORA2A | A2A receptor | Adenosine receptors |
| 20 | ADORA2B | A2B receptor | Adenosine receptors |
| 21 | ADORA3 | A3 receptor | Adenosine receptors |
| 22 | ADRA1A | α1A-adrenoceptor | Adrenoceptors |
| 23 | ADRA1B | α1B-adrenoceptor | Adrenoceptors |
| 24 | ADRA1D | α1D-adrenoceptor | Adrenoceptors |
| 25 | ADRA2A | α2A-adrenoceptor | Adrenoceptors |
| 26 | ADRA2B | α2B-adrenoceptor | Adrenoceptors |
| 27 | ADRA2C | α2C-adrenoceptor | Adrenoceptors |
| 28 | ADRB1 | β1-adrenoceptor | Adrenoceptors |
| 29 | ADRB2 | β2-adrenoceptor | Adrenoceptors |
| 30 | ADRB3 | β3-adrenoceptor | Adrenoceptors |
| 31 | AGTR1 | AT1 receptor | Angiotensin receptors |
| 32 | APLNR | apelin receptor | Apelin receptor |
| 33 | GPBAR1(TGR5) | GPBA receptor | Bile acid receptor |
| 34 | BRS3 | BB3 receptor | Bombesin receptors |
| 35 | GRPR | BB2 receptor | Bombesin receptors |
| 36 | NMBR | BB1 receptor | Bombesin receptors |
| 37 | CALCR | CT receptor | Calcitonin receptors |
| 38 | CALCRL | calcitonin receptor-like receptor | Calcitonin receptors |
| 39 | CASR | CaS receptor | Calcium-sensing receptor |
| 40 | CNR1 | CB1 receptor | Cannabinoid receptors |
| 41 | CNR2 | CB2 receptor | Cannabinoid receptors |
| 42 | GPR119 | GPR119 | Cannabinoid receptors |
| 43 | GPR55 | GPR55 | Cannabinoid receptors |
| 44 | CMKLR1 | chemerin receptor 1 | Chemerin receptors |
| 45 | CCR1 | CCR1 | Chemokine receptors |
| 46 | CCR10 | CCR10 | Chemokine receptors |
| 47 | CCR2 | CCR2 | Chemokine receptors |
| 48 | CCR4 | CCR4 | Chemokine receptors |
| 49 | CCR5 | CCR5 | Chemokine receptors |
| 50 | CCR6 | CCR6 | Chemokine receptors |
| 51 | CCR7 | CCR7 | Chemokine receptors |
| 52 | CCR8 | CCR8 | Chemokine receptors |
| 53 | CCR9 | CCR9 | Chemokine receptors |
| 54 | CX3CR1 | CX3CR1 | Chemokine receptors |
| 55 | CXCR1 | CXCR1 | Chemokine receptors |
| 56 | CXCR2 | CXCR2 | Chemokine receptors |
| 57 | CXCR3 | CXCR3 | Chemokine receptors |
| 58 | CXCR5 | CXCR5 | Chemokine receptors |
| 59 | CXCR6 | CXCR6 | Chemokine receptors |
| 60 | XCR1 | XCR1 | Chemokine receptors |
| 61 | CCKAR | CCK1 receptor | Cholecystokinin receptors |
| 62 | CCKBR | CCK2 receptor | Cholecystokinin receptors |
| 63 | C3AR1 | C3a receptor | Complement peptide receptors |
| 64 | C5AR1 | C5a1 receptor | Complement peptide receptors |
| 65 | CRHR1 | CRF1 receptor | Corticotropin-releasing factor receptors |
| 66 | CRHR2 | CRF2 receptor | Corticotropin-releasing factor receptors |
| 67 | DRD1 | D1 receptor | Dopamine receptors |
| 68 | DRD2 | D2 receptor | Dopamine receptors |
| 69 | DRD3 | D3 receptor | Dopamine receptors |
| 70 | DRD4 | D4 receptor | Dopamine receptors |
| 71 | DRD5 | D5 receptor | Dopamine receptors |
| 72 | EDNRA | ETA receptor | Endothelin receptors |
| 73 | EDNRB | ETB receptor | Endothelin receptors |
| 74 | FPR1 | FPR1 | Formylpeptide receptors |
| 75 | FPR2 | FPR2/ALX | Formylpeptide receptors |
| 76 | FPR3 | FPR3 | Formylpeptide receptors |
| 77 | GPR120 | FFA4 receptor | Free fatty acid receptors |
| 78 | GPR40 | FFA1 receptor | Free fatty acid receptors |
| 79 | GPR41 | FFA3 receptor | Free fatty acid receptors |
| 80 | GPR43 | FFA2 receptor | Free fatty acid receptors |
| 81 | GPR84 | GPR84 | Free fatty acid receptors |
| 82 | GABBR1 | GABAB1 | GABAB receptors |
| 83 | GABBR2 | GABAB2 | GABAB receptors |
| 84 | GALR1 | GAL1 receptor | Galanin receptors |
| 85 | GALR2 | GAL2 receptor | Galanin receptors |
| 86 | GALR3 | GAL3 receptor | Galanin receptors |
| 87 | GHSR | ghrelin receptor | Ghrelin receptor |
| 88 | GCGR | glucagon receptor | Glucagon receptor family |
| 89 | GHRHR | GHRH receptor | Glucagon receptor family |
| 90 | GIPR | GIP receptor | Glucagon receptor family |
| 91 | GLP1R | GLP-1 receptor | Glucagon receptor family |
| 92 | GLP2R | GLP-2 receptor | Glucagon receptor family |
| 93 | SCTR | secretin receptor | Glucagon receptor family |
| 94 | FSHR | FSH receptor | Glycoprotein hormone receptors |
| 95 | LHCGR | LH receptor | Glycoprotein hormone receptors |
| 96 | TSHR | TSH receptor | Glycoprotein hormone receptors |
| 97 | GNRHR | GnRH1 receptor | Gonadotrophin-releasing hormone receptors |
| 98 | HRH1 | H1 receptor | Histamine receptors |
| 99 | HRH2 | H2 receptor | Histamine receptors |
| 100 | HRH3 | H3 receptor | Histamine receptors |
| 101 | HRH4 | H4 receptor | Histamine receptors |
| 102 | GPR109A | HCA2 receptor | Hydroxycarboxylic acid receptors |
| 103 | GPR109B | HCA3 receptor | Hydroxycarboxylic acid receptors |
| 104 | GPR81 | HCA1 receptor | Hydroxycarboxylic acid receptors |
| 105 | KISS1R | kisspeptin receptor | Kisspeptin receptor |
| 106 | CYSLTR1 | CysLT1 receptor | Leukotriene receptors |
| 107 | CYSLTR2 | CysLT2 receptor | Leukotriene receptors |
| 108 | LTB4R | BLT1 receptor | Leukotriene receptors |
| 109 | LTB4R2 | BLT2 receptor | Leukotriene receptors |
| 110 | OXER1(GPR170) | OXE receptor | Leukotriene receptors |
| 111 | LPAR1 | LPA1 receptor | Lysophospholipid (LPA) receptors |
| 112 | LPAR2 | LPA2 receptor | Lysophospholipid (LPA) receptors |
| 113 | LPAR3 | LPA3 receptor | Lysophospholipid (LPA) receptors |
| 114 | LPAR4 | LPA4 receptor | Lysophospholipid (LPA) receptors |
| 115 | LPAR5 | LPA5 receptor | Lysophospholipid (LPA) receptors |
| 116 | LPAR6 | LPA6 receptor | Lysophospholipid (LPA) receptors |
| 117 | MCHR1 | MCH1 receptor | Melanin-concentrating hormone receptors |
| 118 | MCHR2 | MCH2 receptor | Melanin-concentrating hormone receptors |
| 119 | MC1R | MC1 receptor | Melanocortin receptors |
| 120 | MC2R | MC2 receptor | Melanocortin receptors |
| 121 | MC3R | MC3 receptor | Melanocortin receptors |
| 122 | MC4R | MC4 receptor | Melanocortin receptors |
| 123 | MC5R | MC5 receptor | Melanocortin receptors |
| 124 | MTNR1A | MT1 receptor | Melatonin receptors |
| 125 | MTNR1B | MT2 receptor | Melatonin receptors |
| 126 | GRM1 | mGlu1 receptor | Metabotropic glutamate receptors |
| 127 | GRM2 | mGlu2 receptor | Metabotropic glutamate receptors |
| 128 | GRM4 | mGlu4 receptor | Metabotropic glutamate receptors |
| 129 | GRM5 | mGlu5 receptor | Metabotropic glutamate receptors |
| 130 | GRM6 | mGlu6 receptor | Metabotropic glutamate receptors |
| 131 | GRM8 | mGlu8 receptor | Metabotropic glutamate receptors |
| 132 | MLNR | motilin receptor | Motilin receptor |
| 133 | NMUR1 | NMU1 receptor | Neuromedin U receptors |
| 134 | NMUR2 | NMU2 receptor | Neuromedin U receptors |
| 135 | NPFFR1 | NPFF1 receptor | Neuropeptide FF/neuropeptide AF receptors |
| 136 | NPFFR2 | NPFF2 receptor | Neuropeptide FF/neuropeptide AF receptors |
| 137 | NPSR1 | NPS receptor | Neuropeptide S receptor |
| 138 | NPBWR1 | NPBW1 receptor | Neuropeptide W/neuropeptide B receptors |
| 139 | NPBWR2 | NPBW2 receptor | Neuropeptide W/neuropeptide B receptors |
| 140 | NPY1R | Y1 receptor | Neuropeptide Y receptors |
| 141 | NPY2R | Y2 receptor | Neuropeptide Y receptors |
| 142 | NPY4R | Y4 receptor | Neuropeptide Y receptors |
| 143 | NPY5R | Y5 receptor | Neuropeptide Y receptors |
| 144 | NTSR1 | NTS1 receptor | Neurotensin receptors |
| 145 | NTSR2 | NTS2 receptor | Neurotensin receptors |
| 146 | OPRD1 | δ receptor | Opioid receptors |
| 147 | OPRK1 | κ receptor | Opioid receptors |
| 148 | OPRL1 | NOP receptor | Opioid receptors |
| 149 | OPRM1 | μ receptor | Opioid receptors |
| 150 | HCRTR1 | OX1 receptor | Orexin receptors |
| 151 | HCRTR2 | OX2 receptor | Orexin receptors |
| 152 | ACKR1(CCBP1) | ACKR1 | Orphan receptors |
| 153 | ACKR2(CCBP2) | ACKR2 | Orphan receptors |
| 154 | ACKR3(CXCR7) | ACKR3 | Orphan receptors |
| 155 | ACKR4(CCR11) | ACKR4 | Orphan receptors |
| 156 | AGTR2 | AT2 receptor | Orphan receptors |
| 157 | CCRL2 | CCRL2 | Orphan receptors |
| 158 | GPR1 | chemerin receptor 2 | Orphan receptors |
| 159 | GPR101 | GPR101 | Orphan receptors |
| 160 | GPR107 | GPR107 | Orphan receptors |
| 161 | GPR12 | GPR12 | Orphan receptors |
| 162 | GPR132(G2A) | GPR132 | Orphan receptors |
| 163 | GPR135 | GPR135 | Orphan receptors |
| 164 | GPR137 | GPR137 | Orphan receptors |
| 165 | GPR139 | GPR139 | Orphan receptors |
| 166 | GPR141 | GPR141 | Orphan receptors |
| 167 | GPR142 | GPR142 | Orphan receptors |
| 168 | GPR143 | GPR143 | Orphan receptors |
| 169 | GPR146 | GPR146 | Orphan receptors |
| 170 | GPR148 | GPR148 | Orphan receptors |
| 171 | GPR149 | GPR149 | Orphan receptors |
| 172 | GPR15 | GPR15 | Orphan receptors |
| 173 | GPR150 | GPR150 | Orphan receptors |
| 174 | GPR151(GALR4) | GPR151 | Orphan receptors |
| 175 | GPR152 | GPR152 | Orphan receptors |
| 176 | GPR153 | GPR153 | Orphan receptors |
| 177 | GPR156 | GPR156 | Orphan receptors |
| 178 | GPR157 | GPR157 | Orphan receptors |
| 179 | GPR158 | GPR158 | Orphan receptors |
| 180 | GPR160 | GPR160 | Orphan receptors |
| 181 | GPR161 | GPR161 | Orphan receptors |
| 182 | GPR162 | GPR162 | Orphan receptors |
| 183 | GPR17 | GPR17 | Orphan receptors |
| 184 | GPR171 | GPR171 | Orphan receptors |
| 185 | GPR173 | GPR173 | Orphan receptors |
| 186 | GPR174 | GPR174 | Orphan receptors |
| 187 | GPR175 | TPRA1 | Orphan receptors |
| 188 | GPR176 | GPR176 | Orphan receptors |
| 189 | GPR18 | GPR18 | Orphan receptors |
| 190 | GPR182 | GPR182 | Orphan receptors |
| 191 | GPR19 | GPR19 | Orphan receptors |
| 192 | GPR20 | GPR20 | Orphan receptors |
| 193 | GPR21 | GPR21 | Orphan receptors |
| 194 | GPR22 | GPR22 | Orphan receptors |
| 195 | GPR25 | GPR25 | Orphan receptors |
| 196 | GPR26 | GPR26 | Orphan receptors |
| 197 | GPR27 | GPR27 | Orphan receptors |
| 198 | GPR3 | GPR3 | Orphan receptors |
| 199 | GPR30 | GPER | Orphan receptors |
| 200 | GPR31 | GPR31 | Orphan receptors |
| 201 | GPR32 | GPR32 | Orphan receptors |
| 202 | GPR34 | GPR34 | Orphan receptors |
| 203 | GPR35 | GPR35 | Orphan receptors |
| 204 | GPR37 | GPR37 | Orphan receptors |
| 205 | GPR37L1 | GPR37L1 | Orphan receptors |
| 206 | GPR39 | GPR39 | Orphan receptors |
| 207 | GPR4 | GPR4 | Orphan receptors |
| 208 | GPR45 | GPR45 | Orphan receptors |
| 209 | GPR50 | GPR50 | Orphan receptors |
| 210 | GPR52 | GPR52 | Orphan receptors |
| 211 | GPR6 | GPR6 | Orphan receptors |
| 212 | GPR61 | GPR61 | Orphan receptors |
| 213 | GPR62 | GPR62 | Orphan receptors |
| 214 | GPR63 | GPR63 | Orphan receptors |
| 215 | GPR65 | GPR65 | Orphan receptors |
| 216 | GPR68 | GPR68 | Orphan receptors |
| 217 | GPR75 | GPR75 | Orphan receptors |
| 218 | GPR78 | GPR78 | Orphan receptors |
| 219 | GPR82 | GPR82 | Orphan receptors |
| 220 | GPR83 | GPR83 | Orphan receptors |
| 221 | GPR85 | GPR85 | Orphan receptors |
| 222 | GPR87 | GPR87 | Orphan receptors |
| 223 | GPR88 | GPR88 | Orphan receptors |
| 224 | GPRC5A | GPRC5A | Orphan receptors |
| 225 | GPRC5B | GPRC5B | Orphan receptors |
| 226 | GPRC5C | GPRC5C | Orphan receptors |
| 227 | GPRC5D | GPRC5D | Orphan receptors |
| 228 | GPRC6A | GPRC6 receptor | Orphan receptors |
| 229 | LGR4 | LGR4 | Orphan receptors |
| 230 | LGR5 | LGR5 | Orphan receptors |
| 231 | LGR6 | LGR6 | Orphan receptors |
| 232 | MAS1 | MAS1 | Orphan receptors |
| 233 | MAS1L | MAS1L | Orphan receptors |
| 234 | MRGPRD | MRGPRD | Orphan receptors |
| 235 | MRGPRE | MRGPRE | Orphan receptors |
| 236 | MRGPRF | MRGPRF | Orphan receptors |
| 237 | MRGPRG | MRGPRG | Orphan receptors |
| 238 | MRGPRX1 | MRGPRX1 | Orphan receptors |
| 239 | MRGPRX2 | MRGPRX2 | Orphan receptors |
| 240 | MRGPRX3 | MRGPRX3 | Orphan receptors |
| 241 | MRGPRX4 | MRGPRX4 | Orphan receptors |
| 242 | TAAR2 | TAAR2 | Orphan receptors |
| 243 | TAAR5 | TAAR5 | Orphan receptors |
| 244 | TAAR6 | TAAR6 | Orphan receptors |
| 245 | TAAR8 | TAAR8 | Orphan receptors |
| 246 | TAAR9 | TAAR9 | Orphan receptors |
| 247 | OXGR1(GPR80/99) | oxoglutarate receptor | Oxoglutarate receptors |
| 248 | PTH1R | PTH1 receptor | Parathyroid hormone receptors |
| 249 | PTH2R | PTH2 receptor | Parathyroid hormone receptors |
| 250 | PTAFR | PAF receptor | Platelet-activating factor receptor |
| 251 | PROKR1 | PKR1 | Prokineticin receptors |
| 252 | PROKR2 | PKR2 | Prokineticin receptors |
| 253 | PRLHR | PrRP receptor | Prolactin-releasing peptide receptor |
| 254 | PTGDR | DP1 receptor | Prostanoid receptors |
| 255 | PTGDR2 | DP2 receptor | Prostanoid receptors |
| 256 | PTGER1 | EP1 receptor | Prostanoid receptors |
| 257 | PTGER2 | EP2 receptor | Prostanoid receptors |
| 258 | PTGER3 | EP3 receptor | Prostanoid receptors |
| 259 | PTGER4 | EP4 receptor | Prostanoid receptors |
| 260 | PTGFR | FP receptor | Prostanoid receptors |
| 261 | PTGIR | IP receptor | Prostanoid receptors |
| 262 | F2R | PAR1 | Proteinase-activated receptors |
| 263 | F2RL1 | PAR2 | Proteinase-activated receptors |
| 264 | F2RL2 | PAR3 | Proteinase-activated receptors |
| 265 | F2RL3 | PAR4 | Proteinase-activated receptors |
| 266 | QRFPR | QRFP receptor | QRFP receptor |
| 267 | RXFP1 | RXFP1 | Relaxin family peptide receptors |
| 268 | RXFP2 | RXFP2 | Relaxin family peptide receptors |
| 269 | RXFP3 | RXFP3 | Relaxin family peptide receptors |
| 270 | RXFP4 | RXFP4 | Relaxin family peptide receptors |
| 271 | SSTR1 | SST1 receptor | Somatostatin receptors |
| 272 | SSTR2 | SST2 receptor | Somatostatin receptors |
| 273 | SSTR3 | SST3 receptor | Somatostatin receptors |
| 274 | SSTR4 | SST4 receptor | Somatostatin receptors |
| 275 | SSTR5 | SST5 receptor | Somatostatin receptors |
| 276 | GPR183 | GPR183 | Steroid receptors |
| 277 | GPR91 | succinate receptor | Succinate receptor |
| 278 | TACR1 | NK1 receptor | Tachykinin receptors |
| 279 | TACR2 | NK2 receptor | Tachykinin receptors |
| 280 | TACR3 | NK3 receptor | Tachykinin receptors |
| 281 | TRHR | TRH1 receptor | Thyrotropin-releasing hormone receptors |
| 282 | TAAR1 | TA1 receptor | Trace amine receptor |
| 283 | UTS2R | UT receptor | Urotensin receptor |
| 284 | AVPR1A | V1A receptor | Vasopressin and oxytocin receptors |
| 285 | AVPR1B | V1B receptor | Vasopressin and oxytocin receptors |
| 286 | AVPR2 | V2 receptor | Vasopressin and oxytocin receptors |
| 287 | OXTR | OT receptor | Vasopressin and oxytocin receptors |
| 288 | ADCYAP1R1 | PAC1 receptor | VIP and PACAP receptors |
| 289 | VIPR1 | VPAC1 receptor | VIP and PACAP receptors |
| 290 | VIPR2 | VPAC2 receptor | VIP and PACAP receptors |
* The assay mode includes agonist/inverse agonist, antagonist, and PAM/NAM. For orphan receptors, we accept only agonist/inverse agonist.
This product is "Research reagent". It is prohibited to use against humans or animals in medical care, clinical diagnoses, or as food.