Biological Information
Background Information:
Why choose SafetyScreen87:
Based on the industry gold-standard from 2012 recommendations (Bowes et al. Nat Rev Drug Discov , 2012) profiling the 44 targets (24 GPCRs, 8 ion channels, 6 enzymes, 1 Kinase, 3 transporters, 2 nuclear receptors) and enriched in 43 additional targets (mainly GPCRs and ion channels), the SafetyScreen87 is ICH S7A/B aligned for IND-submission.
No. of Assays on Panel:
87
Assays on Panel:
Family
GPCR
Name
NK1 Human Tachykinin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
100
Protein
NK1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
Y1 Human Neuropeptide Y GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
106
Protein
Y1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
delta (DOP) Human Opioid GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
114
Protein
delta (DOP)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
mu (MOP) Human Opioid GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
118
Protein
mu (MOP)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
H2 Human Histamine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
1208
Protein
H2
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Glutamate (Non-Selective) Rat Ion Channel [3H] TCP Binding LeadHunter Assay - FR
Item
124
Protein
NMDA(PCP site)
Organism
Rat
Assay Sub Type
Binding
Family
GPCR
Name
alpha2A Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
13
Protein
alpha2A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT1A Human Serotonin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
131
Protein
5-HT1A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
D2S Human Dopamine GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
1322
Protein
D2
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT2B Human Serotonin GPCR [125I](±)DOI Binding Agonist Radioligand LeadHunter Assay - FR
Item
1333
Protein
5-HT2B
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
alpha2B Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
1344
Protein
alpha2B
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT2C Human Serotonin GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
137
Protein
5-HT2C
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
D2L Human Dopamine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
1405
Protein
D2
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
V1A Human Vasopressin / Oxytocin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
159
Protein
V1A
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Cav1.2 (L-type) Rat Calcium Ion Channel Binding (Verapamil Site) LeadHunter Assay - FR
Item
163
Protein
CaV1.2 (Vera. site)
Organism
Rat
Assay Sub Type
Binding
Family
GPCR
Name
alpha1B Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
1633
Protein
alpha1B
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Cav2.2 (N-type) Rat Calcium Ion Channel Binding Antagonist Radioligand LeadHunter Assay - FR
Item
164
Protein
Cav2.2 (N-type)
Organism
Rat
Assay Sub Type
Binding
Family
Ion Channel
Name
KV (Non-Selective) Rat Potassium Ion Channel [125I] alpha-Dendrotoxin Binding LeadHunter Assay - FR
Item
166
Protein
Kv1.1
Organism
Rat
Assay Sub Type
Binding
Family
Protease
Name
Cathepsin G Human Chymotrypsin Serine Peptidase Enzymatic LeadHunter Assay - FR
Item
179
Protein
Cathepsin G
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
beta1 Human Adrenoceptor GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
18
Protein
beta1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
alpha1D Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
1942
Protein
alpha1D
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
A1 Human Adenosine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
2
Protein
A1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
beta2 Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
20
Protein
beta2
Organism
Human
Assay Sub Type
Binding
Family
Transporter
Name
ATPase (Na+/K+) Pig Brain Enzymatic LeadHunter Assay - FR
Item
2009
Protein
Na/K ATPase
Organism
Pig
Assay Sub Type
Enzymatic
Family
NHR
Name
RARalpha Human Retinoic Acid NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
2084
Protein
RARalpha
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
alpha1A Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
2338
Protein
alpha1A
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
PR Human Progesterone NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
2341
Protein
PR
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
AT1 Human Angiotensin GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
24
Protein
AT1
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
nAChR (alpha4/beta2) Human Ion Channel Binding Agonist Radioligand LeadHunter Assay - FR
Item
3029
Protein
nAChR
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
GABAA (alpha1/beta2/gamma2) Human Ion Channel [3H] Muscimol Binding Agonist Radioligand LeadHunter Assay - FR
Item
3051
Protein
GABAA
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
B2 Human Bradykinin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
33
Protein
B2
Organism
Human
Assay Sub Type
Binding
Family
Protease
Name
ACE Human Angiotensin-Converting Metallo Peptidase Enzymatic LeadHunter Assay - FR
Item
3441
Protein
ACE
Organism
Human
Assay Sub Type
Enzymatic
Family
Enzyme
Name
Monoamine Oxidase B (MAO-B) Human Enzymatic LeadHunter Assay - FR
Item
3477
Protein
MAO-B
Organism
Human
Assay Sub Type
Enzymatic
Family
Transporter
Name
NET Human Norepinephrine Transporter Binding Antagonist Radioligand LeadHunter Assay - FR
Item
355
Protein
NET
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CCR1 Human Chemokine GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
361
Protein
CCR1
Organism
Human
Assay Sub Type
Binding
Family
Enzyme
Name
Acetylcholinesterase Human Enzymatic LeadHunter Assay - FR
Item
363
Protein
AChE
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
CB2 Human Cannabinoid GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
37
Protein
CB2
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
GABAA (Non-Selective) Rat Ion Channel [3H] TBOB Binding Antagonist Radioligand LeadHunter Assay - FR
Item
3817
Protein
GABAA (TBOB site)
Organism
Rat
Assay Sub Type
Binding
Family
GPCR
Name
mGlu5 Human Glutamate (Metabotropic) GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
3844
Protein
mGlu5
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CCK1 (CCKA) Human Cholecystokinin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
39
Protein
CCK1 (CCKA)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
A2A Human Adenosine GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
4
Protein
A2A
Organism
Human
Assay Sub Type
Binding
Family
Enzyme
Name
PDE3A Human Phosphodiesterase Enzymatic LeadHunter Assay - FR
Item
4072
Protein
PDE3A
Organism
Human
Assay Sub Type
Enzymatic
Family
Enzyme
Name
PDE4D2 Human Phosphodiesterase Enzymatic LeadHunter Assay - FR
Item
4077
Protein
PDE4D
Organism
Human
Assay Sub Type
Enzymatic
Family
Ion Channel
Name
hERG Human Potassium Ion Channel [3H] Dofetilide Binding Antagonist Radioligand SafetyScreen - FR
Item
4094
Protein
hERG
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CCK2 (CCKB) Human Cholecystokinin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
41
Protein
CCK2 (CCKB)
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
5-HT3 Human Serotonin Ion Channel Binding Antagonist Radioligand LeadHunter Assay - FR
Item
411
Protein
5-HT3A
Organism
Human
Assay Sub Type
Binding
Family
Enzyme
Name
COX1 Human Cyclooxygenase Enzymatic LeadHunter Assay - FR
Item
4173
Protein
COX1
Organism
Human
Assay Sub Type
Enzymatic
Family
Enzyme
Name
COX2 Human Cyclooxygenase Enzymatic LeadHunter Assay - FR
Item
4186
Protein
COX2
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
CXCR2 (IL-8RB) Human Chemokine GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
419
Protein
CXCR2 (IL-8RB)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
MC4 Human Melanocortin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
420
Protein
MC4
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT1B Human Serotonin GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
4376
Protein
5-HT1B
Organism
Human
Assay Sub Type
Binding
Family
Transporter
Name
SERT Human Serotonin Transporter Binding Antagonist Radioligand LeadHunter Assay - FR
Item
439
Protein
SERT
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
D1 Human Dopamine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
44
Protein
D1
Organism
Human
Assay Sub Type
Binding
Family
Neurotransmitter Metabolism
Name
Monoamine Oxidase A (MAO-A) Rat Binding Antagonist Radioligand LeadHunter Assay - FR
Item
443
Protein
MAO-A
Organism
Rat
Assay Sub Type
Binding
Family
GPCR
Name
kappa (KOP) Human Opioid GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
4461
Protein
kappa (KOP)
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
GABAA (alpha1/beta2/gamma2) Human Ion Channel [3H] Flunitrazepam Binding Agonist Radioligand LeadHunter Assay - FR
Item
4518
Protein
GABAA(BZD site)
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Cav1.2 (L-type) Human Calcium Ion Channel Binding (diltiazem site) (benzothiazepines) LeadHunter Assay - FR
Item
4549
Protein
Cav1.2 (L-type)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
PAF Human Platelet-Activating Factor GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
4569
Protein
PAF
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
GR Human Glucocorticoid NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
469
Protein
GR
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
GABAB (B1b/B2) Human GABAB GPCR Mass Spectrometry Binding Antagonist ligand LeadHunter Assay - FR
Item
4699
Protein
GABAB (B1/B2)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CB1 Human Cannabinoid GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
4708
Protein
CB1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT2A Human Serotonin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
471
Protein
5-HT2A
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Glutamate (Non-Selective) Rat Ion Channel Glycine (Strychnine-Insensitive) Mass Spectrometry Binding LeadHunter Assay - FR
Item
5043
Protein
NMDA(strychine-insensitive site)
Organism
Rat
Assay Sub Type
Binding
Family
Ion Channel
Name
Glycine (Non-Selective) Rat Ion Channel Strychnine Mass Spectrometry Binding LeadHunter Assay - FR
Item
5044
Protein
alpha-1 GlyR
Organism
Rat
Assay Sub Type
Binding
Family
Transporter
Name
Adenosine Guinea Pig Transporter Mass Spectrometry Binding Antagonist Ligand LeadHunter Assay - FR
Item
5113
Protein
SLC29A1
Organism
Guinea Pig
Assay Sub Type
Binding
Family
Transporter
Name
DAT Human Dopamine Transporter Binding Antagonist Radioligand LeadHunter Assay - FR
Item
52
Protein
DAT
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
GluK2 Human Ion Channel [3H] Kainic acid Binding LeadHunter Assay - FR
Item
5379
Protein
Kainate
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
ETA Human Endothelin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
54
Protein
ETA
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
ERalpha Human Estrogen NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
5484
Protein
ERalpha
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Cav1.2 (L-type) Human Calcium Ion Channel Binding (Dihydropyridine Site) LeadHunter Assay - FR
Item
5538
Protein
CaV1.2 (DHP site)
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Sodium Channel Site2 (Non-selective) Rat Ion Channel Batrachotoxin Mass Spectrometry Binding LeadHunter Assay - FR
Item
5572
Protein
Nav1.5
Organism
Rat
Assay Sub Type
Binding
Family
Kinase
Name
Lck Human TK Kinase Enzymatic Radiometric [Km ATP] SafetyScreen - FR
Item
5617
Protein
Lck
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
IR (INSR) Human RTK Kinase Enzymatic Radiometric [Km ATP] SafetyScreen - FR
Item
5623
Protein
IR
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
PKCalpha Human PKC Kinase Enzymatic Radiometric [Km ATP] SafetyScreen - FR
Item
5625
Protein
PKCalpha
Organism
Human
Assay Sub Type
Enzymatic
Family
Transporter
Name
GAT1 Human GABA Transporter Binding Antagonist Radioligand LeadHunter Assay - FR
Item
5773
Protein
GAT-1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CysLT1 Human Leukotriene GPCR Mass Spectrometry Binding Agonist ligand LeadHunter Assay - FR
Item
5841
Protein
CYSLT1
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Glutamate (NMDA, NR1/NR2A) Human Ion Channel [3H] CGP-39653 Binding LeadHunter Assay - FR
Item
5875
Protein
GluN1 / GluN2A
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Glutamate (AMPA, Non-Selective) Rat Ion Channel [3H] AMPA Binding LeadHunter Assay - FR
Item
64
Protein
AMPA
Organism
Rat
Assay Sub Type
Binding
Family
NHR
Name
PPARgamma Human NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
641
Protein
PPARgamma
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
MC1 Mouse Melanocortin GPCR Binding Agonist Radioligand LeadHunter Assay - FR
Item
644
Protein
MC1
Organism
Mouse
Assay Sub Type
Binding
Family
GPCR
Name
H1 Human Histamine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
870
Protein
H1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
M1 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
91
Protein
M1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
M2 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
93
Protein
M2
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
AR Human Androgen NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
933
Protein
AR
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
nAChR (Alpha1, Muscle-Type) Human Ion Channel Binding Antagonist Radioligand LeadHunter Assay - FR
Item
936
Protein
nAChR-α1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
M3 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
95
Protein
M3
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
M4 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
Item
96
Protein
M4
Organism
Human
Assay Sub Type
Binding
Testing Information
Test Sample Requirements:
Minimum for Screen: 130 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing.
(PBS or HBSS working solutions are not compatible)
Turnaround Time
Standard:
10 Business Days
Additional Information
Brand:
SafetyScreen
Testing Location:
France - Celle L'Evescault
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