OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
The SafetyScreen59 Extended Panel provides follow-up screening after the initial SafetyScreen18 Core Panel, evaluating 59 additional safety-related targets, including 33 emerging targets, identified by the IQ DruSafe In vitro Secondary Pharmacology Working Group (Brennan, R.J., et al. Nat Rev Drug Discov, 2024). Predominantly consisting of GPCRs and kinases, these targets show strong associations with both preclinical and clinical adverse effects
No. of Assays on Panel:
59
Assays on Panel:
Family
Epigenetic
Name
BRD4 (BD1) Human Bromodomain-Containing 4 Binding LeadHunter Assay - TW
Item
107800
Protein
BRD4 (BD1)
Organism
Human
Assay Sub Type
Binding
Family
Protease
Name
Cathepsin D Human Pepsin Aspartic Peptidase Enzymatic LeadHunter Assay - TW
Item
112350
Protein
Cathepsin D
Organism
Human
Assay Sub Type
Enzymatic
Family
Lipid Metabolism
Name
COX1 Human Cyclooxygenase Enzymatic LeadHunter Assay - TW
Item
116030
Protein
COX1
Organism
Human
Assay Sub Type
Enzymatic
Family
Lipid Metabolism
Name
COX2 Human Cyclooxygenase Enzymatic LeadHunter Assay - TW
Item
118030
Protein
COX2
Organism
Human
Assay Sub Type
Enzymatic
Family
Oxidoreductase
Name
Monoamine Oxidase A (MAO-A) Human Enzymatic LeadHunter Assay - TW
Item
140010
Protein
MAO-A
Organism
Human
Assay Sub Type
Enzymatic
Family
Oxidoreductase
Name
Monoamine Oxidase B (MAO-B) Human Enzymatic LeadHunter Assay - TW
Item
140120
Protein
MAO-B
Organism
Human
Assay Sub Type
Enzymatic
Family
Protease
Name
MALT1 Human Paracaspase Cysteine Peptidase Enzymatic LeadHunter Assay - TW
Item
164020
Protein
MALT1
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
PI3Kgamma (PIK3CG) (p120gamma) Human PtdIns(4,5)P 3-Kinase Enzymatic ADP-Glo [10 uM ATP] Kinase LeadHunter Assay - TW
Item
167030
Protein
PI3Kgamma
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
PDHK1 Human PDHK Kinase Enzymatic ADP-Glo [10 μM ATP] Kinase LeadHunter Assay - TW
Item
167041
Protein
PDHK1
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
ATM Human PIKK Kinase Enzymatic HTRF [100 μM ATP] Kinase LeadHunter Assay - TW
Item
167070
Protein
ATM
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Aurora-A Human Other Protein Kinase Enzymatic Radiometric Assay [10 μM ATP] - TW
Item
167100
Protein
Aurora-A
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Aurora-B Human Other Protein Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
167130
Protein
Aurora-B
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
EGFR Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
170020
Protein
EGFR
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
ROCK1 Human AGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
171520
Protein
ROCK1
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
ROCK2 Human AGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
171550
Protein
ROCK2
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
CLIK (STK35) Human Other Protein Kinase Enzymatic Radiometric [10 µM ATP] Kinase LeadHunter Assay - TW
Item
171585
Protein
STK35
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
FGFR Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
171790
Protein
FGFR1
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Flt-1 (VEGFR1) Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
171800
Protein
Flt-1 (VEGFR1)
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
KDR (VEGFR2) Human RTK Kinase Enzymatic Radiometric Assay [10 μM ATP] - TW
Item
171820
Protein
KDR (VEGFR2)
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
FAK Human TK Kinase Enzymatic Radiometric Assay [10 μM ATP] - TW
Item
173000
Protein
FAK
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Kit Human RTK Kinase Enzymatic Radiometric Assay [10 μM ATP] - TW
Item
174100
Protein
Kit
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
IR Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
174990
Protein
IR
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
TRKA Human RTK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
175040
Protein
TRKA
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
MAP2K7 (MKK7) Human STE Kinase Enzymatic Radiometric [10 µM ATP] LeadHunter Assay - TW
Item
176115
Protein
MAPKK7
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
GSK3beta Human CMGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
176500
Protein
GSK3beta
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Src Human TK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
Item
176810
Protein
Src
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
A2A Human Adenosine GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
200610
Protein
A2A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
alpha2A Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
203630
Protein
alpha2A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
beta1 Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
204010
Protein
beta1
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
AR Human Androgen NHR Binding Agonist Radioligand LeadHunter Assay - TW
Item
206000
Protein
AR
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CB2 Human Cannabinoid GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
217100
Protein
CB2
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CCK1 (CCKA) Human Cholecystokinin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
218030
Protein
CCK1 (CCKA)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
CCK2 (CCKB) Human Cholecystokinin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
218130
Protein
CCK2 (CCKB)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
D2S Human Dopamine GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
219700
Protein
D2
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
D3 Human Dopamine GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
219800
Protein
D3
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
ETA Human Endothelin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
224010
Protein
ETA
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
ERalpha Human Estrogen NHR Binding Agonist Radioligand LeadHunter Assay - TW
Item
226010
Protein
ERalpha
Organism
Human
Assay Sub Type
Binding
Family
Transporter
Name
GABA (Non-Selective) Rat Transporter Binding Antagonist Radioligand LeadHunter Assay - TW
Item
226400
Protein
Organism
Rat
Assay Sub Type
Binding
Family
NHR
Name
GR Human Glucocorticoid NHR Binding Agonist Radioligand LeadHunter Assay - TW
Item
232030
Protein
GR
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Glutamate (NMDA, NR1/NR2A) Human Ion Channel [3H] CGP-39653 Binding LeadHunter Assay - TW
Item
232820
Protein
GluN1/ GluN2A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
H2 Human Histamine GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
239710
Protein
H2
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
M1 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
252610
Protein
M1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
M2 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
252710
Protein
M2
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
NK3 Human Tachykinin GPCR Binding (Agonist Radioligand) Assay, Panlabs
Item
255710
Protein
NK3
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
nAChR (alpha1) Human Ion Channel Binding Antagonist Radioligand LeadHunter Assay - TW
Item
258700
Protein
nAChR-a1
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
delta (DOP) Human Opioid GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
260130
Protein
delta (DOP)
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
kappa (KOP) Human Opioid GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
260210
Protein
kappa (KOP)
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
Kv1.1 Human Potassium Channel Binding Antagonist Radioligand LeadHunter Assay – TW
Item
265710
Protein
Kv1.1
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
RARalpha Human Retinoic Acid NHR Binding (Agonist Radioligand) Assay, Panlabs
Item
269200
Protein
RARalpha
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT1A Human Serotonin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
271110
Protein
5-HT1A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT1B Human Serotonin GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
271230
Protein
5-HT1B
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT2A Human Serotonin GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
271650
Protein
5-HT2A
Organism
Human
Assay Sub Type
Binding
Family
Ion Channel
Name
5-HT3 Human Serotonin Ion Channel Binding Antagonist Radioligand LeadHunter Assay - TW
Item
271910
Protein
5-HT3A
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
5-HT6 Human Serotonin GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item
272200
Protein
5-HT6
Organism
Human
Assay Sub Type
Binding
Family
Transporter
Name
SERT Human Serotonin Transporter Binding Antagonist Radioligand LeadHunter Assay - TW
Item
274030
Protein
SERT
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
V1A Human Vasopressin / Oxytocin GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
Item
287530
Protein
V1A
Organism
Human
Assay Sub Type
Binding
Family
NHR
Name
PR Human Progesterone NHR Binding Agonist Radioligand LeadHunter Assay - TW
Item
299005
Protein
PR
Organism
Human
Assay Sub Type
Binding
Family
GPCR
Name
GPBA (TGR5) Human Bile Acid GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
304110-0
Protein
GPBAR
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
MRGX2 (MRGPRX2) Human Class A Orphan GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
331840-0
Protein
Mas-related G-protein coupled receptor member X2
Organism
Human
Assay Sub Type
Cell Based
Assay Information
Platform:
Plate reader
Testing Information
Test Concentration / Dose:
Suggested concentration for initial testing is 10 µM
Test Sample Requirements:
210 μL of a 10 mM stock or 1.5 mg pre-weighed powder (assuming FW≦500 and purity 100%)
Turnaround Time
Standard:
10 Business Days
Clinical Relevance
Adverse / Beneficial Action:
Potential adverse effects across multiple organ systems
Additional Information
Brand:
SafetyScreen
Testing Location:
Taiwan - Taipei
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