Biological Information
Background Information:
Why choose SafetyScreen59:
The SafetyScreen59 Functional Extended Panel provides IC₅₀/EC₅₀ -based safety profiling across 59 recommended targets , including 33 emerging ones, with strong representation of GPCRs and kinases, enabling early de-risking and broader detection of potential safety liabilities. It provides follow-up screening after the initial SafetyScreen18 Panel, in order to reach the 77-target safety coverage considered current industry best practices for early off-target risk assessment, as reflected in meta-analysis of Top 20 pharma worldwide under the IQ DruSafe consortium (Brennan et al., Nat Rev Drug Discov , 2024).
The resulting data support safety-margin calculations and earlier risk detection to help advance safer drug candidates.
No. of Assays on Panel:
86
Assays on Panel:
Family
GPCR
Name
V1A Human Vasopressin / Oxytocin GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
1033
Protein
V1A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
V1A Human Vasopressin / Oxytocin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
1034
Protein
V1A
Organism
Human
Assay Sub Type
Cell Based
Family
Lipid Metabolism
Name
COX1 Human Cyclooxygenase Enzymatic LeadHunter Assay - TW
Item
116030
Protein
COX1
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
M1 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
1262
Protein
M1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
ETA Human Endothelin GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
1264
Protein
ETA
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
NK3 Human Tachykinin GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
1312
Protein
NK3
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
M1 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
1474
Protein
M1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
beta1 Human Adrenoceptor GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1605
Protein
beta1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
beta1 Human Adrenoceptor GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1606
Protein
beta1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT6 Human Serotonin GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1627
Protein
5-HT6
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT6 Human Serotonin GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1628
Protein
5-HT6
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
M2 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1658
Protein
M2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
M2 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1659
Protein
M2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
H2 Human Histamine GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1695
Protein
H2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
H2 Human Histamine GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1696
Protein
H2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CB2 Human Cannabinoid GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1746
Protein
CB2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CB2 Human Cannabinoid GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1747
Protein
CB2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
NK3 Human Tachykinin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
1766
Protein
NK3
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CCK1 (CCKA) Human Cholecystokinin GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1876
Protein
CCK1 (CCKA)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CCK1 (CCKA) Human Cholecystokinin GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1877
Protein
CCK1 (CCKA)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1878
Protein
CCK2 (CCKB)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CCK2 (CCKB) Human Cholecystokinin GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1879
Protein
CCK2 (CCKB)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
A2A Rat Adenosine GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
2055
Protein
A2A
Organism
Rat
Assay Sub Type
Cell Based
Family
GPCR
Name
A2A Rat Adenosine GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
2056
Protein
A2A
Organism
Rat
Assay Sub Type
Cell Based
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
ETA Human Endothelin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
2257
Protein
ETA
Organism
Human
Assay Sub Type
Cell Based
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
5-HT2A Human Serotonin GPCR Cell Based Agonist IP1 LeadHunter Assay - FR
Item
3196
Protein
5-HT2A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT2A Human Serotonin GPCR Cell Based Antagonist IP1 LeadHunter Assay - FR
Item
3198
Protein
5-HT2A
Organism
Human
Assay Sub Type
Cell Based
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
GPCR
Name
GPBA (TGR5) Human Bile Acid GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
3998
Protein
TGR5
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
GPBA (TGR5) Human Bile Acid GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
4093
Protein
TGR5
Organism
Human
Assay Sub Type
Cell Based
Family
Enzyme
Name
COX2 Human Cyclooxygenase Enzymatic LeadHunter Assay - FR
Item
4186
Protein
COX2
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
D2L Human Dopamine GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
4253
Protein
D2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
D2L Human Dopamine GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
4254
Protein
D2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
MRGX2 (MRGPRX2) Human Class A Orphan GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
4282
Protein
MRGX2 (MRGPRX2)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
MRGX2 (MRGPRX2) Human Class A Orphan GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
4283
Protein
MRGX2 (MRGPRX2)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
alpha2A Human Adrenoceptor GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
4316
Protein
alpha2A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
alpha2A Human Adrenoceptor GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
4317
Protein
alpha2A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
delta (DOP) Human Opioid GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
4328
Protein
delta (DOP)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
delta (DOP) Human Opioid GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
4329
Protein
delta (DOP)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT1A Human Serotonin GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
4332
Protein
5-HT1A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT1A Human Serotonin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
4333
Protein
5-HT1A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT1B Human Serotonin GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
4385
Protein
5-HT1B
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT1B Human Serotonin GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
4386
Protein
5-HT1B
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
kappa (KOP) Human Opioid GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
4459
Protein
kappa (KOP)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
kappa (KOP) Human Opioid GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
4460
Protein
kappa (KOP)
Organism
Human
Assay Sub Type
Cell Based
Family
Transporter
Name
SERT Human Serotonin Transporter Functional Antagonist Uptake LeadHunter Assay - FR
Item
4864
Protein
SERT
Organism
Human
Assay Sub Type
Cell Based
Family
Enzyme
Name
Monoamine Oxidase A (MAO-A) Human Enzymatic LeadHunter Assay - FR
Item
5108
Protein
MAO-A
Organism
Human
Assay Sub Type
Enzymatic
Family
Epigenetic
Name
BRD4 (1) Human Bromodomain-Containing 4 Binding LeadHunter Assay - FR
Item
5716
Protein
BRD4
Organism
Human
Assay Sub Type
Binding
Family
Enzyme
Name
MALT1 Human Protease Enzymatic Fluorimetry LeadHunter Assay - FR
Item
5717
Protein
MALT1
Organism
Human
Assay Sub Type
Enzymatic
Family
Ion Channel
Name
5-HT3a Human Serotonin Ion Channel Functional Cell Based Agonist Calcium Flux LeadHunter Assay - FR
Item
5742
Protein
5-HT3A
Organism
Human
Assay Sub Type
Cell Based
Family
Ion Channel
Name
5-HT3a Human Serotonin Ion Channel Functional Cell Based Antagonist Calcium Flux LeadHunter Assay - FR
Item
5746
Protein
5-HT3A
Organism
Human
Assay Sub Type
Cell Based
Family
NHR
Name
ERalpha Human Estrogen NHR Cell Based Agonist Reporter LeadHunter Assay - FR
Item
5747
Protein
ERalpha
Organism
Human
Assay Sub Type
Cell Based
Family
NHR
Name
GR Human Glucocorticoid NHR Cell Based Agonist Reporter LeadHunter Assay - FR
Item
5748
Protein
GR
Organism
Human
Assay Sub Type
Cell Based
Family
Transporter
Name
GAT1 Human GABA Transporter Functional Antagonist Uptake LeadHunter Assay - FR
Item
5774
Protein
GAT-1
Organism
Human
Assay Sub Type
Cell Based
Family
Kinase
Name
MKK7 (MAP2K7) Human Kinase STE Enzymatic [Km ATP] SafetyScreen - FR
Item
5814
Protein
MAPKK 7
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
ATM Human PIKK Kinase Enzymatic [1mM ATP] SafetyScreen - FR
Item
5891
Protein
ATM
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Aurora-A (AURKA) Human Other Protein Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5892
Protein
Aurora-A
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Aurora-B (AURKB) Human Other Protein Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5893
Protein
Aurora-B
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
c-Kit Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5894
Protein
Kit
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
CLIK (STK35) Human Other Protein Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5895
Protein
CLIK
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
EGFR Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5896
Protein
EGFR
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
FAK Human TK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5897
Protein
FAK
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
TRKA Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5898
Protein
TRKA
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
FGFR1 Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5899
Protein
FGFR1
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Src Human TK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5900
Protein
Src
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
ROCK2 Human AGC Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5901
Protein
ROCK2
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
ROCK1 Human AGC Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5902
Protein
ROCK1
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
Flt-1 (VEGFR1) (FLT1) Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5903
Protein
Flt-1 (VEGFR1)
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
PI3Kgamma (PIK3CG) (p120gamma) Human PtdIns(4,5)P 3-Kinase Enzymatic [1mM ATP] SafetyScreen - FR
Item
5904
Protein
PI3Kgamma
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
GSK3beta (GSK3B) Human CMGC Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5905
Protein
GSK3beta
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
KDR (VEGFR2) (KDR) Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5906
Protein
KDR (VEGFR2)
Organism
Human
Assay Sub Type
Enzymatic
Family
Kinase
Name
IR (INSR) Human RTK Kinase Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5907
Protein
IR
Organism
Human
Assay Sub Type
Enzymatic
Family
Ion Channel
Name
Glutamate (NMDA, NR1/NR2A) Human Ion Channel Cell Based Agonist LeadHunter Assay - FR
Item
5916
Protein
GluN2A
Organism
Human
Assay Sub Type
Cell Based
Family
Ion Channel
Name
Glutamate (NMDA, NR1/NR2A) Human Ion Channel Cell Based Antagonist LeadHunter Assay - FR
Item
5917
Protein
GluN2A
Organism
Human
Assay Sub Type
Cell Based
Family
NHR
Name
ERalpha Human Estrogen NHR Cell Based Antagonist Reporter LeadHunter Assay - FR
Item
5919
Protein
ERalpha
Organism
Human
Assay Sub Type
Cell Based
Family
NHR
Name
GR Human Glucocorticoid NHR Cell Based Antagonist Reporter LeadHunter Assay - FR
Item
5920
Protein
GR
Organism
Human
Assay Sub Type
Cell Based
Family
Kinase
Name
PDHK1 (PDK1) Human Kinase Other protein Enzymatic Radiometric [1mM ATP] SafetyScreen - FR
Item
5925
Protein
PDK1
Organism
Human
Assay Sub Type
Enzymatic
Family
Ion Channel
Name
KCNQ1 KvLQT1/minK Human Potassium Ion Channel Thallium Flux Cell Based Antagonist LeadHunter - FR
Item
5941
Protein
KCNQ1
Organism
Human
Assay Sub Type
Cell Based
Family
Ion Channel
Name
nAChR (Alpha1, Muscle-Type) Human Acetylcholine (Nicotinic) Ion Channel Cell Based Agonist LeadHunter Assay - FR
Item
5949
Protein
nAChR a1
Organism
Human
Assay Sub Type
Cell Based
Family
Ion Channel
Name
nAChR (Alpha1, Muscle-Type) Human Acetylcholine (Nicotinic) Ion Channel Cell Based Antagonist LeadHunter Assay - FR
Item
5950
Protein
nAChR a1
Organism
Human
Assay Sub Type
Cell Based
Family
Enzyme
Name
Cathepsin D Human Pepsin Aspartic Peptidase Enzymatic LeadHunter Assay - FR
Item
650
Protein
Cathepsin D
Organism
Human
Assay Sub Type
Enzymatic
Family
GPCR
Name
D3 Human Dopamine GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
683
Protein
D3
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
D3 Human Dopamine GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
684
Protein
D3
Organism
Human
Assay Sub Type
Cell Based
Family
NHR
Name
AR Human Androgen NHR Binding Agonist Radioligand LeadHunter Assay - FR
Item
933
Protein
AR
Organism
Human
Assay Sub Type
Binding
Testing Information
Test Sample Requirements:
500 µL of a 333× DMSO stock solution, calculated from the top concentration to be tested (PBS working solutions are not compatible)
Turnaround Time
Standard:
15 Business Days
Additional Information
Brand:
SafetyScreen
Testing Location:
France - Celle L'Evescault
Other Information:
Available on demand in single-concentration screening format. Contact us for more information : ClientServicesPoitiers@discovery.eurofinseu.com
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