Reaction BiologyおよびEuroscrrenFAST (former Euroscreen)では、GPCR、イオンチャネル、トランスポーター、CYP等、ヒトにおいて薬物有害反応を引き起こす可能性のある幅広いターゲットに対する、化合物のオフターゲットスクリーニングに有用なパネルアッセイを提供しています。新薬開発の早い段階での安全性評価等にご利用いただけます。

  • Euroscreen Safety Panel (45ターゲット)
  • Reaction Biology In Vitro Evaluation of Safety and Toxicity (InVEST) panel (53ターゲット)

Safety panel (Euroscreen)

45種のGPCR、トランスポーター、イオンチャネル、各種酵素のパネルです。
Target familyTarget nameSpecies / Cell LineAssay / Tracer
1GPCRAdenosine A2AHumancAMP
2GPCRAdrenergic alpha1aHumancAMP
3GPCRAdrenergic alpha2aHumancAMP
4GPCRAdrenergic beta2HumancAMP
5GPCRCannabinoid CB1HumanGTP
6GPCRCholecystokinin CCK1HumanAEQ
7GPCRDopamine D1HumancAMP
8GPCRDopamine D2SHumancAMP
9GPCREndothelin ETAHumanAEQ
10GPCREndothelin ETBHumanAEQ
11GPCRHistamine H1HumanAEQ
12GPCRHistamine H2HumancAMP
13GPCRMelatonin MT1HumanGTP
14GPCRMelatonin MT2HumanGTP
15GPCRMuscarinic M1HumanAEQ
16GPCRMuscarinic M2HumancAMP
17GPCROpioid deltaHumancAMP
18GPCROpioid kappaHumancAMP
19GPCROpioid muHumancAMP
20GPCRSerotonine 5-HT1AHumancAMP
21GPCRSerotonine 5-HT1BHumancAMP
22GPCRSerotonine 5-HT2AHumanIPOne
23GPCRSerotonine 5-HT2BHumanIPOne
24GPCRSerotonine 5-HT3HumanAEQ
25GPCRVasopressin V1aHumanAEQ
26Acetylcholin esteraseAChEElectric EelFluorescence
27CyclooxygenaseCOX-2HumanColorimetric
28Monoamine OxidaseMAO-AHumanLuminescence
29PhosphodiesterasePDE-3HumanHTRF
30PhosphodiesterasePDE-4HumanHTRF
31Cytochrome P4501A2HumanLuminescence
32Cytochrome P4502C9HumanLuminescence
33Cytochrome P4502D6HumanLuminescence
34Cytochrome P4502E1HumanLuminescence
35Cytochrome P4503A4HumanLuminescence
36Amine TransporterDATCHO-K1[3H]-WIN 35,428
37Amine TransporterNETHEK293[3H]-Nisoxetine
38Amine TransporterSERTU2OS[3H]-Citalopram
39Ion ChannelCa2+ channel L, DHP siterat brain[3H]-Nitrendipine
40Ion ChannelCa2+ channel L, verapamil siterat brain[N-methyl-3H]-Desmethoxyverapamil
41Ion ChannelhERGHEK293[3H]-Dofetilide
42Ion ChannelGABA BZD (central)rat brain[3H]-Flunitrazepam
43Ion ChannelNMDA (Glutamate) GRIN 1HEK293[3H]-MDL 105,519
44Ion ChannelNicotinic alpha4beta2rat brain[3H]-Cytisine
45SigmaSigmaMCF-7[3H]-Pentazocine

In Vitro Evaluation of Safety and Toxicity (InVEST) panel

53種のGPCR、トランスポーター、イオンチャネル、CYP450、各種酵素等のパネルです。
Target familyTarget nameSpeciesAssay format
1Biogenic Amine TransporterSET (Serotonin Transporter)HumanRadioligand Filter Binding
2Biogenic Amine TransporterDAT (sodium-dependent dopamine transporter)HumanRadioligand Filter Binding
3Biogenic Amine TransporterNET (norepinephrine transporter)HumanRadioligand Filter Binding
4CholinesteraseAcetylcholinesteraseHumanEnzymatic Activity
5CyclooxygenaseCOX-1OvineEnzymatic Activity
6CyclooxygenaseCOX-2HumanEnzymatic Activity
7Cytochrome P450CYP1A2HumanEnzymatic Activity
8Cytochrome P450CYP2A6HumanEnzymatic Activity
9Cytochrome P450CYP2B6HumanEnzymatic Activity
10Cytochrome P450CYP2C19HumanEnzymatic Activity
11Cytochrome P450CYP2C8HumanEnzymatic Activity
12Cytochrome P450CYP2C9HumanEnzymatic Activity
13Cytochrome P450CYP2D6HumanEnzymatic Activity
14Cytochrome P450CYP2E1HumanEnzymatic Activity
15Cytochrome P450CYP2J2HumanEnzymatic Activity
16Cytochrome P450CYP3A4HumanEnzymatic Activity
17Cytochrome P450CYP3A5HumanEnzymatic Activity
18GPCRAdenosine A1 ReceptorHumanRadioligand Filter Binding
19GPCRAdrenergic Alpha 1A ReceptorHumanRadioligand Filter Binding
20GPCRAdrenergic Alpha 2A ReceptorHumanRadioligand Filter Binding
21GPCRAdrenergic Beta 1HumanRadioligand Filter Binding
22GPCRAdrenergic Beta 2HumanRadioligand Filter Binding
23GPCRCCK1 ReceptorHumanRadioligand Filter Binding
24GPCRDopamine D1 ReceptorHumanRadioligand Filter Binding
25GPCRDopamine D2S ReceptorHumanRadioligand Filter Binding
26GPCRDopamine D3 ReceptorHumanRadioligand Filter Binding
27GPCRHistamine H1 ReceptorHumanRadioligand Filter Binding
28GPCRMuscarinic M1 ReceptorHumanRadioligand Filter Binding
29GPCRMuscarinic M2 ReceptorHumanRadioligand Filter Binding
30GPCRMuscarinic M3 ReceptorHumanRadioligand Filter Binding
31GPCRMuscarinic M4 ReceptorHumanRadioligand Filter Binding
32GPCRMuscarinic M5 ReceptorHumanRadioligand Filter Binding
33GPCROpioid delta ReceptorHumanRadioligand Filter Binding
34GPCROpioid kappa ReceptorHumanRadioligand Filter Binding
35GPCROpioid mu ReceptorHumanRadioligand Filter Binding
36GPCRSerotonin 5-HT1A ReceptorHumanRadioligand Filter Binding
37GPCRSerotonin 5-HT1B ReceptorHumanRadioligand Filter Binding
38Ion ChannelhERGHumanFluorescence Polarization
39Ion ChannelCentral BDZ (GABA-A Receptor)RatRadioligand Filter Binding
40Ion Channel5-HT3HumanRadioligand Filter Binding
41Monoamine oxidaseMAO-AHumanEnzymatic Activity
42Monoamine oxidaseMAO-BHumanEnzymatic Activity
43Nuclear ReceptorEstrogen Receptor aHumanFluorescence Polarization
44Nuclear ReceptorGlucocorticoid ReceptorHumanFluorescence Polarization
45Nuclear ReceptorPPARg ReceptorHumanFluorescence Polarization
46Nuclear ReceptorProgesterone ReceptorHumanFluorescence Polarization
47PhosphodiesterasePDE3AHumanEnzymatic Activity
48PhosphodiesterasePDE4AHumanEnzymatic Activity
49PhosphodiesterasePDE4DHumanEnzymatic Activity
50PhosphodiesterasePDE4D2HumanEnzymatic Activity
51ProteaseACE-1HumanEnzymatic Activity
52ProteaseCathepsin GHumanEnzymatic Activity
53ProteaseThrombin AlphaHumanEnzymatic Activity