Epics Therapeutics (former Euroscreen)のEuroscreenFASTでは、各種疾患に焦点を当てたパネルや各受容体ファミリーのパネルアッセイを提供しています。GPCRパネルアッセイの多くは、各GPCRに対してナチュラルなGタンパク質のカップリングステータスに基づいた測定法を採用しており、化合物のアゴニスト及びアンタゴニスト活性の測定を行います。
- 57 GPCR Diversity panel (57)
- CNS panel (36)
- Metabolic panel (54)
- Inflammation panel (56)
- Sensory Pain panel (41)
- Metabotropic Glutamate (mGlu) receptors panel (8)
- Muscarinic receptors panel (5)
- Serotonin receptors panel (14)
- Chemokine receptors panel (21)
- Orphan receptors panel (76)
57 GPCR Diversity panel
主要な受容体ファミリーを代表する57 GPCRの幅広いパネルです。 | Target name | Assay method |
|---|
| 1 | Serotonin 5-HT1A | cAMP |
| 2 | Serotonin 5-HT1B | cAMP |
| 3 | Serotonin 5-HT2A | AEQ |
| 4 | Serotonin 5-HT2B | AEQ |
| 5 | Serotonin 5-HT2Cne | AEQ |
| 6 | Serotonin 5-HT3 | AEQ |
| 7 | Serotonin 5-HT4e | cAMP |
| 8 | Serotonin 5-HT5a | AEQ |
| 9 | Serotonin 5-HT6 | cAMP |
| 10 | Serotonin 5-HT7 | cAMP |
| 11 | Adenosine A1 | cAMP |
| 12 | Adenosine A2A | cAMP |
| 13 | Adenosine A3 | cAMP |
| 14 | Adrenergic beta1 | cAMP |
| 15 | Adrenergic beta2 | cAMP |
| 16 | Adrenergic alpha1A | AEQ |
| 17 | Adrenergic alpha1B | AEQ |
| 18 | Adrenergic alpha2A | GTPgS |
| 19 | Adrenergic alpha2B | GTPgS |
| 20 | Adrenergic alpha2C | GTPgS |
| 21 | Angiotensin AT1 | AEQ |
| 22 | Bradykinin B1 | AEQ |
| 23 | Cannabinoid CB1 | cAMP |
| 24 | Cannabinoid CB2 | cAMP |
| 25 | Cholecystokinin CCK1 | AEQ |
| 26 | Cholecystokinin CCK2 | AEQ |
| 27 | Calcitonin CGRP | AEQ |
| 28 | Chemokine CXCR1 | GTPgS |
| 29 | Leukotrien CysLT1 | AEQ |
| 30 | Dopamine D1 | cAMP |
| 31 | Dopamine D2 | GTPgS |
| 32 | Dopamine D3 | GTPgS |
| 33 | Dopamine D4.4 | GTPgS |
| 34 | Endothelin ETA | AEQ |
| 35 | Endothelin ETB | AEQ |
| 36 | Ghrelin GHS-R | AEQ |
| 37 | Histamine H1 | AEQ |
| 38 | Histamine H2 | cAMP |
| 39 | Histamine H3 | GTPgS |
| 40 | Motilin MTL | AEQ |
| 41 | Muscarinic M1 | AEQ |
| 42 | Muscarinic M2 | GTPgS |
| 43 | Muscarinic M3 | AEQ |
| 44 | Muscarinic M4 | GTPgS |
| 45 | Muscarinic M5 | AEQ |
| 46 | Nociceptin OFQ (NOP) | GTPgS |
| 47 | Neurokinin NK1 | AEQ |
| 48 | Neurokinin NK2 | AEQ |
| 49 | Neuropeptide NPY1 | cAMP |
| 50 | Opioid OP1 | GTPgS |
| 51 | Opioid OP2 | GTPgS |
| 52 | Opioid OP3 | GTPgS |
| 53 | Somatostatin sst4 | GTPgS |
| 54 | Urotensin-II | AEQ |
| 55 | Vasopressin V1a | AEQ |
| 56 | Vasopressin V1b | AEQ |
| 57 | VPAC1 | AEQ |
CNS panel
CNSに焦点を当てた36 GPCRのパネルです。 | Target name | Assay method |
|---|
| 1 | Serotonin 5-HT1A | GTPgS |
| 2 | Serotonin 5-HT2A | AEQ |
| 3 | Serotonin 5-HT2Ce | AEQ |
| 4 | Adenosine A1 | cAMP |
| 5 | Adrenergic alpha1B | AEQ |
| 6 | Adrenergic alpha2A | cAMP |
| 7 | Bombesin B2 | AEQ |
| 8 | Cannabinoid CB1 | cAMP |
| 9 | Cholecystokinin CCK2 | AEQ |
| 10 | Corticotropin CRF1 | cAMP |
| 11 | Corticotropin CRF2b | cAMP |
| 12 | Dopamine D1 | cAMP |
| 13 | Dopamine D2L | cAMP |
| 14 | Galanin GAL2 | AEQ |
| 15 | Histamine H1 | AEQ |
| 16 | Histamine H3 | GTPgS |
| 17 | MCH1 | AEQ |
| 18 | mGluR2 | cAMP |
| 19 | Muscarinic M1 | AEQ |
| 20 | Muscarinic M2 | GTPgS |
| 21 | Muscarinic M3 | AEQ |
| 22 | Muscarinic M4 | GTPgS |
| 23 | Muscarinic M5 | AEQ |
| 24 | Nociceptin OFQ (NOP) | GTPgS |
| 25 | Neurokinin NK1 | AEQ |
| 26 | Neurokinin NK2 | AEQ |
| 27 | Neuropeptide NPY2 | AEQ |
| 28 | Neurotensin NT1 | AEQ |
| 29 | Opioid OP1 | GTPgS |
| 30 | Opioid OP2 | GTPgS |
| 31 | Opioid OP3 | GTPgS |
| 32 | Orexin OX1 | AEQ |
| 33 | Orexin OX2 | AEQ |
| 34 | Somatostatin sst2 | GTPgS |
| 35 | Vasopressin V1b | AEQ |
| 36 | PAC1 | AEQ |
Metabolic panel
代謝調節や疾患に関与する54 GPCRのパネルです。 | Target name | Assay method |
|---|
| 1 | Serotonin 5-HT2Ce | AEQ |
| 2 | Adenosine A1 | cAMP |
| 3 | Adenosine A2B | cAMP |
| 4 | Adrenergic beta3 | cAMP |
| 5 | Adrenergic alpha1B | AEQ |
| 6 | Adrenergic alpha2A | cAMP |
| 7 | Angiotensin AT1 | AEQ |
| 8 | Bombesin BB1 | AEQ |
| 9 | Bombesin BB2 | AEQ |
| 10 | Bombesin BB3 | AEQ |
| 11 | Bradykinin B2 | AEQ |
| 12 | Calcitonin CGRP | AEQ |
| 13 | Calcium CaS | AEQ |
| 14 | Cannabinoid CB1 | GTPgS |
| 15 | Cannabinoid CB2 | GTPgS |
| 16 | Chemokine CCR2b | GTPgS |
| 17 | Chemokine CCR4 | GTPgS |
| 18 | Chemokine CXCR3 | GTPgS |
| 19 | Cholecystokinin CCK1 | AEQ |
| 20 | Corticotropin CRF2b | cAMP |
| 21 | FFA1 /GPR40 | AEQ |
| 22 | FFA2 / GPR43 | cAMP |
| 23 | Galanin GAL2 | AEQ |
| 24 | GIP | cAMP |
| 25 | GLP-1 | cAMP |
| 26 | Glucagon | cAMP |
| 27 | GPR7 | GTPgS |
| 28 | Histamine H1 | AEQ |
| 29 | Histamine H3 | GTPgS |
| 30 | MCH1 | AEQ |
| 31 | MC4 | cAMP |
| 32 | MC5 | cAMP |
| 33 | Muscarinic M1 | AEQ |
| 34 | Muscarinic M2 | GTPgS |
| 35 | Muscarinic M3 | AEQ |
| 36 | NMUR1 | AEQ |
| 37 | Neuropeptide NPY2 | AEQ |
| 38 | Neurotensin NT1 | AEQ |
| 39 | Niacin receptor | cAMP |
| 40 | Nociceptin OFQ (NOP) | GTPgS |
| 41 | Opioid OP2 | GTPgS |
| 42 | Opioid OP3 | GTPgS |
| 43 | Orexin OX1 | AEQ |
| 44 | Orexin OX2 | AEQ |
| 45 | Oxytocin OT1 | AEQ |
| 46 | Prokineticin PKR2 | AEQ |
| 47 | Prostanoid EP2 | cAMP |
| 48 | PTH1 | cAMP |
| 49 | Secretin | cAMP |
| 50 | Somatostatin sst2 | GTPgS |
| 51 | Urotensin-II | AEQ |
| 52 | Vasopressin V1a | AEQ |
| 53 | PAC1 | AEQ |
| 54 | VPAC2 | AEQ |
Inflammation panel
免疫反応や炎症に関与する56 GPCRのパネルです。 | Target name | Assay method |
|---|
| 1 | Serotonin 5-HT2A | AEQ |
| 2 | Adenosine A1 | cAMP |
| 3 | Adenosine A2A | cAMP |
| 4 | Adenosine A3 | cAMP |
| 5 | Complement C3a | GTPgS |
| 6 | Complement C5a | GTPgS |
| 7 | Bombesin BB1 | AEQ |
| 8 | Bombesin BB2 | AEQ |
| 9 | Bradykinin B2 | AEQ |
| 10 | Calcitonin CGRP | AEQ |
| 11 | Cannabinoid CB2 | cAMP |
| 12 | Chemokine CCR1 | GTPgS |
| 13 | Chemokine CCR2b | AEQ |
| 14 | Chemokine CCR3 | AEQ |
| 15 | Chemokine CCR4 | AEQ |
| 16 | Chemokine CCR5 | AEQ |
| 17 | Chemokine CCR6 | AEQ |
| 18 | Chemokine CCR7 | AEQ |
| 19 | Chemokine CCR8 | AEQ |
| 20 | Chemokine CCR9a | AEQ |
| 21 | Chemokine CCR10 | AEQ |
| 22 | Chemokine CXCR2 | AEQ |
| 23 | Chemokine CXCR3a | AEQ |
| 24 | Chemokine CXCR4 | AEQ |
| 25 | Chemokine XCR1 | AEQ |
| 26 | Free Fatty Acid GPR43 | cAMP |
| 27 | Histamine H1 | AEQ |
| 28 | Histamine H2 | cAMP |
| 29 | Hydroxy Carboxylic Acid GPR109a | AEQ |
| 30 | Leukotrien BLT1 | AEQ |
| 31 | Leukotrien CysLT1 | AEQ |
| 32 | Leukotrien CysLT2 | AEQ |
| 33 | Muscarinic M2 | GTPgS |
| 34 | Muscarinic M4 | GTPgS |
| 35 | Neurokinin NK1 | AEQ |
| 36 | Neuromedin U NMU-1R | AEQ |
| 37 | Neurotensin NTS1 | AEQ |
| 38 | Opioid OP1 | GTPgS |
| 39 | Opioid OP2 | GTPgS |
| 40 | Opioid OP3 | GTPgS |
| 41 | Platelet Activating Factor PAF | cAMP |
| 42 | Prokineticin PKR1 | AEQ |
| 43 | Prostanoid DP | cAMP |
| 44 | Prostanoid EP1 | AEQ |
| 45 | Prostanoid EP3 | AEQ |
| 46 | Prostanoid EP4 | cAMP |
| 47 | Prostanoid IP1 | cAMP |
| 48 | Protease-activated PAR2 | AEQ |
| 49 | Protease-activated PAR4 | AEQ |
| 50 | Sphingosine S1P1 | AEQ |
| 51 | Sphingosine S1P2 | AEQ |
| 52 | Sphingosine S1P4 | AEQ |
| 53 | Sphingosine S1P5 | AEQ |
| 54 | PAC1 | AEQ |
| 55 | VPAC1 | AEQ |
| 56 | VPAC2 | AEQ |
Sensory Pain panel
感覚痛・疼痛に関与する41のGPCRとイオンチャネルのパネルです。 | Target name | Assay method |
|---|
| 1 | Serotonin 5-HT1A | GTPgS |
| 2 | Serotonin 5-HT2Ce | AEQ |
| 3 | Adenosine A1 | cAMP |
| 4 | Adenosine A3 | cAMP |
| 5 | Adrenergic beta2 | cAMP |
| 6 | Adrenergic alpha2A | cAMP |
| 7 | Bradykinin B2 | AEQ |
| 8 | Cannabinoid CB1 | cAMP |
| 9 | Cannabinoid CB2 | cAMP |
| 10 | Chemokine CCR2b | GTPgS |
| 11 | Chemokine CX3CR1 | GTPgS |
| 12 | Cholecystokinin CCK2 | AEQ |
| 13 | Calcitonin CGRP | AEQ |
| 14 | Galanin GAL1 | GTPgS |
| 15 | GABAB1a/B2 | cAMP |
| 16 | Glutamate mGlu2 | cAMP |
| 17 | Histamine H1 | AEQ |
| 18 | Histamine H3 | GTPgS |
| 19 | MAS related MrgX2 | AEQ |
| 20 | 5-HT3 | AEQ |
| 21 | NMDA GRIN-1 | RLB |
| 22 | Muscarinic M1 | AEQ |
| 23 | Muscarinic M2 | GTPgS |
| 24 | Muscarinic M3 | AEQ |
| 25 | Muscarinic M5 | AEQ |
| 26 | Nociceptin OFQ (NOP) | GTPgS |
| 27 | Neurokinin NK1 | AEQ |
| 28 | Neurokinin NK2 | AEQ |
| 29 | NeuromedinNMU2 | AEQ |
| 30 | Neuropeptide GPR7 | GTPgS |
| 31 | Neurotensin NTS1 | AEQ |
| 32 | Opioid OP1 | GTPgS |
| 33 | Opioid OP2 | GTPgS |
| 34 | Opioid OP3 | GTPgS |
| 35 | Orexin OX1 | AEQ |
| 36 | Parathyroid Hormone PTH1 | cAMP |
| 37 | Platelet-Activating PAF | cAMP |
| 38 | Prokineticin PKR1 | AEQ |
| 39 | Protease Activated PAR2 | GTPgS |
| 40 | TRPA1 | AEQ |
| 41 | TRPV1 | IPOne |
Metabotropic Glutamate (mGlu) receptors panel
8つのmGlu受容体に対して化合物のプロファイリングを行います。 | Target name | Assay method |
|---|
| 1 | mGluR1 | AEQ |
| 2 | mGluR2 | cAMP |
| 3 | mGluR3 | AEQ |
| 4 | mGluR4 | GTPgS |
| 5 | mGluR5 | AEQ |
| 6 | mGluR6 | GTPgS |
| 7 | mGluR7 | cAMP |
| 8 | mGluR8 | GTPgS |
Muscarinic receptors panel
5つのムスカリン受容体に対して化合物のプロファイリングを行います。 | Target name | Assay method |
|---|
| 1 | M1 | AEQ |
| 2 | M2 | GTPgS |
| 3 | M3 | AEQ |
| 4 | M4 | GTPgS |
| 5 | M5 | AEQ |
Serotonin receptors panel
14種類のセロトニン受容体サブタイプに対して化合物のプロファイリングを行います。 | Target name | Assay method |
|---|
| 1 | Serotonin 5-HT1A | GTPgS |
| 2 | Serotonin 5-HT1B | GTPgS |
| 3 | Serotonin 5-HT1D | GTPgS |
| 4 | Serotonin 5-HT1E | GTPgS |
| 5 | Serotonin 5-HT1F | GTPgS |
| 6 | Serotonin 5-HT2A | IPOne |
| 7 | Serotonin 5-HT2B | IPOne |
| 8 | Serotonin 5-HT2Ce | IPOne |
| 9 | Serotonin 5-HT2Cne | IPOne |
| 10 | Serotonin 5-HT3 | AEQ |
| 11 | Serotonin 5-HT4e | cAMP |
| 12 | Serotonin 5-HT5 | AEQ |
| 13 | Serotonin 5-HT6 | cAMP |
| 14 | Serotonin 5-HT7 | cAMP |
Chemokine receptors panel
21種類のヒトケモカイン受容体に対して化合物のプロファイリングを行います。 | Target name | Assay method |
|---|
| 1 | Chemokine CCR1 | GTPgS |
| 2 | Chemokine CCR2 | AEQ |
| 3 | Chemokine CCR3 | AEQ |
| 4 | Chemokine CCR4 | AEQ |
| 5 | Chemokine CCR5 | AEQ |
| 6 | Chemokine CCR6 | AEQ |
| 7 | Chemokine CCR7 | AEQ |
| 8 | Chemokine CCR8 | AEQ |
| 9 | Chemokine CCR9a | AEQ |
| 10 | Chemokine CCR10 | AEQ |
| 11 | Chemokine ChemR23 | AEQ |
| 12 | Chemokine CXCR1 | AEQ |
| 13 | Chemokine CXCR2 | AEQ |
| 14 | Chemokine CXCR3a | AEQ |
| 15 | Chemokine CXCR3b | AEQ |
| 16 | Chemokine CXCR4 | AEQ |
| 17 | Chemokine CXCR5 | AEQ |
| 18 | Chemokine CXCR6 | AEQ |
| 19 | Chemokine CXCR7 | RLB |
| 20 | Chemokine CX3CR1 | AEQ |
| 21 | Chemokine XCR1 | AEQ |
Orphan receptors panel
76のオーファン受容体に対して化合物のプロファイリングを行います。 | Target name | Assay method |
|---|
| 1 | GPR3 | cAMP |
| 2 | GPR4 | cAMP |
| 3 | GPR6 | cAMP |
| 4 | GPR12 | cAMP |
| 5 | GPR17 | cAMP |
| 6 | GPR18 | AEQ |
| 7 | GPR19 (GPR-NGA) | AEQ |
| 8 | GPR20 | AEQ |
| 9 | GPR21 | cAMP |
| 10 | GPR22 | AEQ |
| 11 | GPR23 (LPAR4) | AEQ |
| 12 | GPR25 | AEQ |
| 13 | GPR26 | cAMP |
| 14 | GPR27 (SREB1) | AEQ |
| 15 | GPR30 (GPER) | AEQ |
| 16 | GPR31 | AEQ |
| 17 | GPR32 | AEQ |
| 18 | GPR34 | cAMP |
| 19 | GPR35 | cAMP |
| 20 | GPR37 | AEQ |
| 21 | GPR37L1 | AEQ |
| 22 | GPR39 | AEQ |
| 23 | GPR45 | AEQ |
| 24 | GPR50 | AEQ |
| 25 | GPR52 | cAMP |
| 26 | GPR55 | AEQ |
| 27 | GPR61 | cAMP |
| 28 | GPR62 | cAMP |
| 29 | GPR63 | AEQ |
| 30 | GPR65 | cAMP |
| 31 | GPR68 (OGR1) | IPOne |
| 32 | GPR75 | AEQ |
| 33 | GPR78 | cAMP |
| 34 | GPR82 | AEQ |
| 35 | GPR83 (GPR72) | AEQ |
| 36 | GPR84 | cAMP |
| 37 | GPR87 (HG03) | IPOne |
| 38 | GPR88 | cAMP |
| 39 | GPR91 | AEQ |
| 40 | GPR99 | AEQ |
| 41 | GPR101 | cAMP |
| 42 | GPR139 | AEQ |
| 43 | GPR141 | AEQ |
| 44 | GPR142 | IPOne |
| 45 | GPR146 | AEQ |
| 46 | GPR148 | AEQ |
| 47 | GPR149 | AEQ |
| 48 | GPR150 | AEQ |
| 49 | GPR151 | AEQ |
| 50 | GPR152 | AEQ |
| 51 | GPR153 | AEQ |
| 52 | GPR161 (RE2) | cAMP |
| 53 | GPR162 (A-2) | AEQ |
| 54 | GPR171 (H963) | AEQ |
| 55 | GPR173 (SREB3) | AEQ |
| 56 | GPR174 (DA6) | AEQ |
| 57 | GPR176 (HB954) | AEQ |
| 58 | GPR182 (HSGPCP) | AEQ |
| 59 | GPRC5A (RAIG1) | AEQ |
| 60 | GPRC5B (RAIG2) | AEQ |
| 61 | GPRC5C (RAIG3) | AEQ |
| 62 | GPRC5D (RAIG4) | AEQ |
| 63 | LPA5 (GPR92) | IPOne |
| 64 | MAS | AEQ |
| 65 | MRG | AEQ |
| 66 | MRGD | AEQ |
| 67 | MRGE | AEQ |
| 68 | MRGF (RTA) | AEQ |
| 69 | P2Y5 | AEQ |
| 70 | P2Y8 | AEQ |
| 71 | P2Y10 | AEQ |
| 72 | TAAR2 (GPR58) | cAMP |
| 73 | TAAR5 (PNR) | cAMP |
| 74 | TAAR6 (TA4) | cAMP |
| 75 | TAAR8 (TA5) | cAMP |
| 76 | TAAR9 (TA3) | cAMP |
