Biochemical Assay - Safety Panel Assays -

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 44 (InVEST44) panel (44ターゲット)
Reaction Biology In Vitro Safety Pharmacology Target [InVEST44 panelに追加可能] (55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 family	Target name	Species / Cell Line	Assay / Tracer
1	GPCR	Adenosine A2A	Human	cAMP
2	GPCR	Adrenergic alpha1a	Human	cAMP
3	GPCR	Adrenergic alpha2a	Human	cAMP
4	GPCR	Adrenergic beta2	Human	cAMP
5	GPCR	Cannabinoid CB1	Human	GTP
6	GPCR	Cholecystokinin CCK1	Human	AEQ
7	GPCR	Dopamine D1	Human	cAMP
8	GPCR	Dopamine D2S	Human	cAMP
9	GPCR	Endothelin ETA	Human	AEQ
10	GPCR	Endothelin ETB	Human	AEQ
11	GPCR	Histamine H1	Human	AEQ
12	GPCR	Histamine H2	Human	cAMP
13	GPCR	Melatonin MT1	Human	GTP
14	GPCR	Melatonin MT2	Human	GTP
15	GPCR	Muscarinic M1	Human	AEQ
16	GPCR	Muscarinic M2	Human	cAMP
17	GPCR	Opioid delta	Human	cAMP
18	GPCR	Opioid kappa	Human	cAMP
19	GPCR	Opioid mu	Human	cAMP
20	GPCR	Serotonine 5-HT1A	Human	cAMP
21	GPCR	Serotonine 5-HT1B	Human	cAMP
22	GPCR	Serotonine 5-HT2A	Human	IPOne
23	GPCR	Serotonine 5-HT2B	Human	IPOne
24	GPCR	Serotonine 5-HT3	Human	AEQ
25	GPCR	Vasopressin V1a	Human	AEQ
26	Acetylcholin esterase	AChE	Electric Eel	Fluorescence
27	Cyclooxygenase	COX-2	Human	Colorimetric
28	Monoamine Oxidase	MAO-A	Human	Luminescence
29	Phosphodiesterase	PDE-3	Human	HTRF
30	Phosphodiesterase	PDE-4	Human	HTRF
31	Cytochrome P450	1A2	Human	Luminescence
32	Cytochrome P450	2C9	Human	Luminescence
33	Cytochrome P450	2D6	Human	Luminescence
34	Cytochrome P450	2E1	Human	Luminescence
35	Cytochrome P450	3A4	Human	Luminescence


36	Amine Transporter	DAT	CHO-K1	[³H]-WIN 35,428
37	Amine Transporter	NET	HEK293	[³H]-Nisoxetine
38	Amine Transporter	SERT	U2OS	[³H]-Citalopram
39	Ion Channel	Ca2+ channel L, DHP site	rat brain	[³H]-Nitrendipine
40	Ion Channel	Ca2+ channel L, verapamil site	rat brain	[N-methyl-³H]-Desmethoxyverapamil
41	Ion Channel	hERG	HEK293	[³H]-Dofetilide
42	Ion Channel	GABA BZD (central)	rat brain	[³H]-Flunitrazepam
43	Ion Channel	NMDA (Glutamate) GRIN 1	HEK293	[³H]-MDL 105,519
44	Ion Channel	Nicotinic alpha4beta2	rat brain	[³H]-Cytisine
45	Sigma	Sigma	MCF-7	[³H]-Pentazocine

In Vitro Evaluation of Safety and Toxicity (InVEST) 44 panel

44種のGPCR、トランスポーター、イオンチャネル、各種酵素等のパネルです。

	Target family	Target name	Species	Assay format
1	GPCR	Adenosine A2A	Human	Radioligand Filter Binding
2	GPCR	Adrenergic α1A	Human	Radioligand Filter Binding
3	GPCR	Adrenergic α2A	Human	Radioligand Filter Binding
4	GPCR	Adrenergic β1A	Human	Radioligand Filter Binding
5	GPCR	Adrenergic β2A	Human	Radioligand Filter Binding
6	GPCR	Cannabinoid CB1	Human	Radioligand Filter Binding
7	GPCR	Cannabinoid CB2	Human	Radioligand Filter Binding
8	GPCR	Cholecystokinin CCK1	Human	Radioligand Filter Binding
9	GPCR	Dopamine D1	Human	Radioligand Filter Binding
10	GPCR	Dopamine D2S	Human	Radioligand Filter Binding
11	GPCR	Histamine H1	Human	Radioligand Filter Binding
12	GPCR	Muscarinic M1	Human	Radioligand Filter Binding
13	GPCR	Muscarinic M2	Human	Radioligand Filter Binding
14	GPCR	Muscarinic M3	Human	Radioligand Filter Binding
15	GPCR	Opioid (δ)	Human	Radioligand Filter Binding
16	GPCR	Opioid (κ)	Human	Radioligand Filter Binding
17	GPCR	Opioid (μ)	Human	Radioligand Filter Binding
18	GPCR	Serotonin 5-HT1A	Human	Radioligand Filter Binding
19	GPCR	Serotonin 5-HT1B	Human	Radioligand Filter Binding
20	GPCR	Serotonin 5-HT2A	Human	Radioligand Filter Binding
21	GPCR	Serotonin 5-HT2B	Human	Radioligand Filter Binding
22	GPCR	Endothelin ETA	Human	FLIPR/Ca Assay
23	GPCR	Histamine H2	Human	Radioligand Binding
24	GPCR	Vasopressin V1A	Human	Cell Reporter
25	Ion Channel	Serotonin 5-HT3	Human	Radioligand Filter Binding
26	Ion Channel	GABAA	Rat	Radioligand Filter Binding
27	Ion Channel	hERG	Human	Fluorescence Polarization
28	Ion Channel	NMDA	Rat	Radioligand Filter Binding
29	Ion Channel	Cav1.2	Human	Patch Clamp
30	Ion Channel	nAChR (α4/β2)	Human	FLIPR/Ca Assay
31	Ion Channel	Nav1.5	Human	Patch Clamp
32	Kinase	LCK TK	Human	Enzymatic Activity
33	Monoamine oxidase	MAO-A	Human	Enzymatic Activity
34	Monoamine oxidase	MAO-B	Human	Enzymatic Activity
35	Phosphodiesterase	PDE3A	Human	Enzymatic Activity
36	Phosphodiesterase	PDE4D2	Human	Enzymatic Activity
37	Other Enzymes	Acetylcholinesterase	Human	Enzymatic Activity
38	Cyclooxygenase	COX1	Ovine	Enzymatic Activity
39	Cyclooxygenase	COX2	Human	Enzymatic Activity
40	Transporter	Dopamine DAT	Human	Radioligand Filter Binding
41	Transporter	Norepinephrine NET	Human	Radioligand Filter Binding
42	Transporter	Serotonin SERT	Human	Radioligand Filter Binding
43	Nuclear Receptor	Glucocorticoid	Human	Fluorescence Polarization
44	Nuclear Receptor	Androgen	Human	Cell Reporter

In Vitro Safety Pharmacology Target

53種のGPCR、トランスポーター、イオンチャネル、CYP450、各種酵素等から選んで、上記InVEST44 panelアッセイに追加して試験を行うことも可能です。

	Target family	Target name	Species	Assay format
1	Cytochrome P450	CYP1A2	Human	Enzymatic Activity
2	Cytochrome P450	CYP2A6	Human	Enzymatic Activity
3	Cytochrome P450	CYP2B6	Human	Enzymatic Activity
4	Cytochrome P450	CYP2C8	Human	Enzymatic Activity
5	Cytochrome P450	CYP2C9	Human	Enzymatic Activity
6	Cytochrome P450	CYP2C19	Human	Enzymatic Activity
7	Cytochrome P450	CYP2D6	Human	Enzymatic Activity
8	Cytochrome P450	CYP2E1	Human	Enzymatic Activity
9	Cytochrome P450	CYP2J2	Human	Enzymatic Activity
10	Cytochrome P450	CYP3A4 (BOMCC)	Human	Enzymatic Activity
11	Cytochrome P450	CYP3A5	Human	Enzymatic Activity
12	Cytochrome P450	CYP4A11	Human	Enzymatic Activity
13	Cytochrome P450	CYP4F3B	Human	Enzymatic Activity
14	Cytochrome P450	CYP19A	Human	Enzymatic Activity
15	GPCR	Adenosine A1	Human	Radioligand Filter Binding
16	GPCR	Adrenergic α1A	Human	FLIPR/Ca Assay
17	GPCR	Cannabinoid CB1	Human	FLIPR/Ca Assay
18	GPCR	Dopamine D1	Human	Envision/cAMP Assay
19	GPCR	Dopamine D3	Human	Radioligand Filter Binding
20	GPCR	Histamine H1	Human	FLIPR/Ca Assay
21	GPCR	Histamine H2	Human	FLIPR/Ca Assay
22	GPCR	Muscarinic M3	Human	FLIPR/Ca Assay
23	GPCR	Muscarinic M4	Human	Radioligand Filter Binding
24	GPCR	Muscarinic M5	Human	Radioligand Filter Binding
25	GPCR	Opioid (δ)	Human	FLIPR/Ca Assay
26	GPCR	Opioid (κ)	Human	FLIPR/Ca Assay
27	GPCR	Opioid (μ)	Human	FLIPR/Ca Assay
28	GPCR	Serotonin 5-HT2A	Human	FLIPR/Ca Assay
29	GPCR	Serotonin 5-HT2B	Human	FLIPR/Ca Assay
30	Ion Channel	hERG	Human	Patch Clamp
31	Nuclear Receptor	Estrogen-α	Human	Fluorescence Polarization
32	Nuclear Receptor	Estrogen-α	Human	Cell Reporter
33	Nuclear Receptor	Glucocorticoid	Human	Cell Reporter
34	Nuclear Receptor	PPARgamma	Human	Fluorescence Polarization
35	Nuclear Receptor	Progesterone PR	Human	Fluorescence Polarization
36	Nuclear Receptor	Progesterone PR	Human	Cell Reporter
37	Phosphodiesterase	PDE1A	Human	Enzymatic Activity
38	Phosphodiesterase	PDE1B	Human	Enzymatic Activity
39	Phosphodiesterase	PDE1C	Human	Enzymatic Activity
40	Phosphodiesterase	PDE2A	Human	Enzymatic Activity
41	Phosphodiesterase	PDE3B	Human	Enzymatic Activity
42	Phosphodiesterase	PDE4A	Human	Enzymatic Activity
43	Phosphodiesterase	PDE4B	Human	Enzymatic Activity
44	Phosphodiesterase	PDE4C	Human	Enzymatic Activity
45	Phosphodiesterase	PDE4D	Human	Enzymatic Activity
46	Phosphodiesterase	PDE5A	Human	Enzymatic Activity
47	Phosphodiesterase	PDE7A	Human	Enzymatic Activity
48	Phosphodiesterase	PDE7B	Human	Enzymatic Activity
49	Phosphodiesterase	PDE8A	Human	Enzymatic Activity
50	Phosphodiesterase	PDE9A	Human	Enzymatic Activity
51	Phosphodiesterase	PDE10A	Human	Enzymatic Activity
52	Protease	ACE-1	Human	Enzymatic Activity
53	Protease	Cathepsin G	Human	Enzymatic Activity
54	Protease	Thrombin Alpha	Human	Enzymatic Activity
55	Transporter	Dopamine DAT	Human	FLIPR/NT Assay