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 nameAssay method
1Serotonin 5-HT1AcAMP
2Serotonin 5-HT1BcAMP
3Serotonin 5-HT2AAEQ
4Serotonin 5-HT2BAEQ
5Serotonin 5-HT2CneAEQ
6Serotonin 5-HT3AEQ
7Serotonin 5-HT4ecAMP
8Serotonin 5-HT5aAEQ
9Serotonin 5-HT6cAMP
10Serotonin 5-HT7cAMP
11Adenosine A1cAMP
12Adenosine A2AcAMP
13Adenosine A3cAMP
14Adrenergic beta1cAMP
15Adrenergic beta2cAMP
16Adrenergic  alpha1AAEQ
17Adrenergic  alpha1BAEQ
18Adrenergic  alpha2AGTPgS
19Adrenergic  alpha2BGTPgS
20Adrenergic  alpha2CGTPgS
21Angiotensin AT1AEQ
22Bradykinin B1AEQ
23Cannabinoid CB1cAMP
24Cannabinoid CB2cAMP
25Cholecystokinin CCK1AEQ
26Cholecystokinin CCK2AEQ
27Calcitonin CGRPAEQ
28Chemokine CXCR1GTPgS
29Leukotrien CysLT1AEQ
30Dopamine D1cAMP
31Dopamine D2GTPgS
32Dopamine D3GTPgS
33Dopamine D4.4GTPgS
34Endothelin ETAAEQ
35Endothelin ETBAEQ
36Ghrelin GHS-RAEQ
37Histamine H1AEQ
38Histamine H2cAMP
39Histamine H3GTPgS
40Motilin MTLAEQ
41Muscarinic M1AEQ
42Muscarinic M2GTPgS
43Muscarinic M3AEQ
44Muscarinic M4GTPgS
45Muscarinic M5AEQ
46Nociceptin OFQ (NOP)GTPgS
47Neurokinin NK1AEQ
48Neurokinin NK2AEQ
49Neuropeptide NPY1cAMP
50Opioid OP1GTPgS
51Opioid OP2GTPgS
52Opioid OP3GTPgS
53Somatostatin sst4GTPgS
54Urotensin-IIAEQ
55Vasopressin V1aAEQ
56Vasopressin V1bAEQ
57VPAC1AEQ

CNS panel

CNSに焦点を当てた36 GPCRのパネルです。
Target nameAssay method
1Serotonin 5-HT1AGTPgS
2Serotonin 5-HT2AAEQ
3Serotonin 5-HT2CeAEQ
4Adenosine A1cAMP
5Adrenergic  alpha1BAEQ
6Adrenergic  alpha2AcAMP
7Bombesin B2AEQ
8Cannabinoid CB1cAMP
9Cholecystokinin CCK2AEQ
10Corticotropin CRF1cAMP
11Corticotropin CRF2bcAMP
12Dopamine D1cAMP
13Dopamine D2LcAMP
14Galanin GAL2AEQ
15Histamine H1AEQ
16Histamine H3GTPgS
17MCH1AEQ
18mGluR2cAMP
19Muscarinic M1AEQ
20Muscarinic M2GTPgS
21Muscarinic M3AEQ
22Muscarinic M4GTPgS
23Muscarinic M5AEQ
24Nociceptin OFQ (NOP)GTPgS
25Neurokinin NK1AEQ
26Neurokinin NK2AEQ
27Neuropeptide NPY2AEQ
28Neurotensin NT1AEQ
29Opioid OP1GTPgS
30Opioid OP2GTPgS
31Opioid OP3GTPgS
32Orexin OX1AEQ
33Orexin OX2AEQ
34Somatostatin sst2GTPgS
35Vasopressin V1bAEQ
36PAC1AEQ

Metabolic panel

代謝調節や疾患に関与する54 GPCRのパネルです。
Target nameAssay method
1Serotonin 5-HT2CeAEQ
2Adenosine A1cAMP
3Adenosine A2BcAMP
4Adrenergic beta3cAMP
5Adrenergic  alpha1BAEQ
6Adrenergic  alpha2AcAMP
7Angiotensin AT1AEQ
8Bombesin BB1AEQ
9Bombesin BB2AEQ
10Bombesin BB3AEQ
11Bradykinin B2AEQ
12Calcitonin CGRPAEQ
13Calcium CaSAEQ
14Cannabinoid CB1GTPgS
15Cannabinoid CB2GTPgS
16Chemokine CCR2bGTPgS
17Chemokine CCR4GTPgS
18Chemokine CXCR3GTPgS
19Cholecystokinin CCK1AEQ
20Corticotropin CRF2bcAMP
21FFA1 /GPR40AEQ
22FFA2 / GPR43cAMP
23Galanin GAL2AEQ
24GIPcAMP
25GLP-1cAMP
26GlucagoncAMP
27GPR7GTPgS
28Histamine H1AEQ
29Histamine H3GTPgS
30MCH1AEQ
31MC4cAMP
32MC5cAMP
33Muscarinic M1AEQ
34Muscarinic M2GTPgS
35Muscarinic M3AEQ
36NMUR1AEQ
37Neuropeptide NPY2AEQ
38Neurotensin NT1AEQ
39Niacin receptorcAMP
40Nociceptin OFQ (NOP)GTPgS
41Opioid OP2GTPgS
42Opioid OP3GTPgS
43Orexin OX1AEQ
44Orexin OX2AEQ
45Oxytocin OT1AEQ
46Prokineticin PKR2AEQ
47Prostanoid EP2cAMP
48PTH1cAMP
49SecretincAMP
50Somatostatin sst2GTPgS
51Urotensin-IIAEQ
52Vasopressin V1aAEQ
53PAC1AEQ
54VPAC2AEQ

Inflammation panel

免疫反応や炎症に関与する56 GPCRのパネルです。
Target nameAssay method
1Serotonin 5-HT2AAEQ
2Adenosine A1cAMP
3Adenosine A2AcAMP
4Adenosine A3cAMP
5Complement C3aGTPgS
6Complement C5aGTPgS
7Bombesin BB1AEQ
8Bombesin BB2AEQ
9Bradykinin B2AEQ
10Calcitonin CGRPAEQ
11Cannabinoid CB2cAMP
12Chemokine CCR1GTPgS
13Chemokine CCR2bAEQ
14Chemokine CCR3AEQ
15Chemokine CCR4AEQ
16Chemokine CCR5AEQ
17Chemokine CCR6AEQ
18Chemokine CCR7AEQ
19Chemokine CCR8AEQ
20Chemokine CCR9aAEQ
21Chemokine CCR10AEQ
22Chemokine CXCR2AEQ
23Chemokine CXCR3aAEQ
24Chemokine CXCR4AEQ
25Chemokine XCR1AEQ
26Free Fatty Acid GPR43cAMP
27Histamine H1AEQ
28Histamine H2cAMP
29Hydroxy Carboxylic Acid GPR109aAEQ
30Leukotrien BLT1AEQ
31Leukotrien CysLT1AEQ
32Leukotrien CysLT2AEQ
33Muscarinic M2GTPgS
34Muscarinic M4GTPgS
35Neurokinin NK1AEQ
36Neuromedin U NMU-1RAEQ
37Neurotensin NTS1AEQ
38Opioid OP1GTPgS
39Opioid OP2GTPgS
40Opioid OP3GTPgS
41Platelet Activating Factor PAFcAMP
42Prokineticin PKR1AEQ
43Prostanoid DPcAMP
44Prostanoid EP1AEQ
45Prostanoid EP3AEQ
46Prostanoid EP4cAMP
47Prostanoid IP1cAMP
48Protease-activated PAR2AEQ
49Protease-activated PAR4AEQ
50Sphingosine S1P1AEQ
51Sphingosine S1P2AEQ
52Sphingosine S1P4AEQ
53Sphingosine S1P5AEQ
54PAC1AEQ
55VPAC1AEQ
56VPAC2AEQ

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 nameAssay method
1Serotonin 5-HT1AGTPgS
2Serotonin 5-HT2CeAEQ
3Adenosine A1cAMP
4Adenosine A3cAMP
5Adrenergic beta2cAMP
6Adrenergic  alpha2AcAMP
7Bradykinin B2AEQ
8Cannabinoid CB1cAMP
9Cannabinoid CB2cAMP
10Chemokine CCR2bGTPgS
11Chemokine CX3CR1GTPgS
12Cholecystokinin CCK2AEQ
13Calcitonin CGRPAEQ
14Galanin GAL1GTPgS
15GABAB1a/B2cAMP
16Glutamate mGlu2cAMP
17Histamine H1AEQ
18Histamine H3GTPgS
19MAS related MrgX2AEQ
205-HT3AEQ
21NMDA GRIN-1RLB
22Muscarinic M1AEQ
23Muscarinic M2GTPgS
24Muscarinic M3AEQ
25Muscarinic M5AEQ
26Nociceptin OFQ (NOP)GTPgS
27Neurokinin NK1AEQ
28Neurokinin NK2AEQ
29NeuromedinNMU2AEQ
30Neuropeptide GPR7GTPgS
31Neurotensin NTS1AEQ
32Opioid OP1GTPgS
33Opioid OP2GTPgS
34Opioid OP3GTPgS
35Orexin OX1AEQ
36Parathyroid Hormone PTH1cAMP
37Platelet-Activating PAFcAMP
38Prokineticin PKR1AEQ
39Protease Activated PAR2GTPgS
40TRPA1AEQ
41TRPV1IPOne

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 nameAssay method
1mGluR1AEQ
2mGluR2cAMP
3mGluR3AEQ
4mGluR4GTPgS
5mGluR5AEQ
6mGluR6GTPgS
7mGluR7cAMP
8mGluR8GTPgS

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 nameAssay method
1M1AEQ
2M2GTPgS
3M3AEQ
4M4GTPgS
5M5AEQ

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 nameAssay method
1Serotonin 5-HT1AGTPgS
2Serotonin 5-HT1BGTPgS
3Serotonin 5-HT1DGTPgS
4Serotonin 5-HT1EGTPgS
5Serotonin 5-HT1FGTPgS
6Serotonin 5-HT2AIPOne
7Serotonin 5-HT2BIPOne
8Serotonin 5-HT2CeIPOne
9Serotonin 5-HT2CneIPOne
10Serotonin 5-HT3AEQ
11Serotonin 5-HT4ecAMP
12Serotonin 5-HT5AEQ
13Serotonin 5-HT6cAMP
14Serotonin 5-HT7cAMP

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 nameAssay method
1Chemokine CCR1GTPgS
2Chemokine CCR2AEQ
3Chemokine CCR3AEQ
4Chemokine CCR4AEQ
5Chemokine CCR5AEQ
6Chemokine CCR6AEQ
7Chemokine CCR7AEQ
8Chemokine CCR8AEQ
9Chemokine CCR9aAEQ
10Chemokine CCR10AEQ
11Chemokine ChemR23AEQ
12Chemokine CXCR1AEQ
13Chemokine CXCR2AEQ
14Chemokine CXCR3aAEQ
15Chemokine CXCR3bAEQ
16Chemokine CXCR4AEQ
17Chemokine CXCR5AEQ
18Chemokine CXCR6AEQ
19Chemokine CXCR7RLB
20Chemokine CX3CR1AEQ
21Chemokine XCR1AEQ

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 nameAssay method
1GPR3cAMP
2GPR4cAMP
3GPR6cAMP
4GPR12cAMP
5GPR17cAMP
6GPR18AEQ
7GPR19 (GPR-NGA)AEQ
8GPR20AEQ
9GPR21cAMP
10GPR22AEQ
11GPR23 (LPAR4)AEQ
12GPR25AEQ
13GPR26cAMP
14GPR27 (SREB1)AEQ
15GPR30 (GPER)AEQ
16GPR31AEQ
17GPR32AEQ
18GPR34cAMP
19GPR35cAMP
20GPR37AEQ
21GPR37L1AEQ
22GPR39AEQ
23GPR45AEQ
24GPR50AEQ
25GPR52cAMP
26GPR55AEQ
27GPR61cAMP
28GPR62cAMP
29GPR63AEQ
30GPR65cAMP
31GPR68 (OGR1)IPOne
32GPR75AEQ
33GPR78cAMP
34GPR82AEQ
35GPR83 (GPR72)AEQ
36GPR84cAMP
37GPR87 (HG03)IPOne
38GPR88cAMP
39GPR91AEQ
40GPR99AEQ
41GPR101cAMP
42GPR139AEQ
43GPR141AEQ
44GPR142IPOne
45GPR146AEQ
46GPR148AEQ
47GPR149AEQ
48GPR150AEQ
49GPR151AEQ
50GPR152AEQ
51GPR153AEQ
52GPR161 (RE2)cAMP
53GPR162 (A-2)AEQ
54GPR171 (H963)AEQ
55GPR173 (SREB3)AEQ
56GPR174 (DA6)AEQ
57GPR176 (HB954)AEQ
58GPR182 (HSGPCP)AEQ
59GPRC5A (RAIG1)AEQ
60GPRC5B (RAIG2)AEQ
61GPRC5C (RAIG3)AEQ
62GPRC5D (RAIG4)AEQ
63LPA5 (GPR92)IPOne
64MASAEQ
65MRGAEQ
66MRGDAEQ
67MRGEAEQ
68MRGF (RTA)AEQ
69P2Y5AEQ
70P2Y8AEQ
71P2Y10AEQ
72TAAR2 (GPR58)cAMP
73TAAR5 (PNR)cAMP
74TAAR6 (TA4)cAMP
75TAAR8 (TA5)cAMP
76TAAR9 (TA3)cAMP