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SAFETYscanIn Vitro Pharmacological Profiling Services

In vitro pharmacological profiling is increasingly being used earlier in the drug discovery process to identify undesirable off-target activity profiles. SAFETYscan offers a broad menu, including the assays recommended by major pharmaceutical companies (Bowes et.al. 2012). All of the SAFETYscan assays are human orthologs and provide functional data for cell surface receptors, while other commercial panels are primarily binding assays for humans and rodents. Assessing the specificity of lead compounds early in development using highly relevant and predictive assays allows more informed decisions about compound safety, ultimately leading to the development of safer and more effective drugs.

SAFETYscan In Vitro Pharmacological Profiling Services Highlights
 
  • Save resources by identifying potential adverse events before expensive animal studies or clinical trials
  • Reach actionable data faster by reducing false positives with functional readouts
  • Improve data quality with mechanism of action data from agonist and antagonist mode

Learn more about SAFETYscan Ion Channel Services.

Safety47™ panel of  functional assays with all human targets for safety screening – Available Now


       Inquire                Information Sheet
 
FamilyGene SymbolTargetReadout
AdrenoceptorsADRA2AADRA2AcAMP
AdrenoceptorsADRB1ADRB1cAMP
AdrenoceptorsADRB2ADRB2cAMP
CannabinoidCNR1CB1cAMP
CannabinoidCNR2CB2cAMP
CholecystokininCCKARCCK1Calcium
DopamineDRD1D1cAMP
DopamineDRD2SD2ScAMP
EndothelinEDNRAETACalcium
HistamineHRH1H1Calcium
HistamineHRH2H2cAMP
AcetylcholineCHRM1M1Calcium
AcetylcholineCHRM2M2cAMP
AcetylcholineCHRM3M3Calcium
OpioidOPRD1OPRD1cAMP
OpioidOPRK1OPRK1cAMP
OpioidOPRM1OPRM1cAMP
5-HydroxytryptamineHTR1A5HT1AcAMP
5-HydroxytryptamineHTR1B5HT1BcAMP
5-HydroxytryptamineHTR2A5HT2ACalcium
5-HydroxytryptamineHTR2B5HT2BCalcium
Vasopressin and OxytocinAVPR1AAVPR1ACalcium
AdenosineADORA2AADORA2ACalcium
AdrenoceptorsADRA1AADRA1ACalcium
GABA receptorGABRA1GABAAMembrane potential
Serotonin receptorHTR3A5-HT3Calcium flux
Calcium channelCACNA1CCAv1.2Calcium flux
Potassium channelKCNH2hERGThallium flux
Sodium channelSCN5ANAv1.5Membrane potential
Glutamate channelNMDAR 1A/2BGRIN1/GRIN2BCalcium flux
Potassium channelKVLQT1/minKKCNQ1Thallium flux
Nicotinic channelnAChR(a4/b2)CHRNA4/CHRNB2Calcium flux
TKINSRINSRKINOMEscan
TKVEGFR2VEGFR2KINOMEscan
AGCROCK1ROCK1KINOMEscan
TKLCKLCKKINOMEscan
CyclooxygenaseCOX1COX1Enzymatic activity
CyclooxygenaseCOX2COX2Enzymatic activity
CholinesteraseAChEAChEEnzymatic activity
Monoamine oxidaseMAOAMAO-AEnzymatic activity
PhosphodiesterasePDE3APDE3AEnzymatic activity
PhosphodiesterasePDE4D2PDE4D2Enzymatic Activity
NHRARARNuclear translocation
NHRGRGRProtein interaction
DopamineSLC6A3DATNeurotransmitter uptake
NorepinephrineSLC6A2NETNeurotransmitter uptake
5-HydroxytryptamineSLC6A4SERTNeurotransmitter uptake

For additional GPCR targets, please click here

For additional kinase targets, please click here

Inhibition of Serotonin (5-Hydroxytryptamine) HTR2B by Reference Compounds

HTR2B Antagonist SAFETYscan Image

Cells were stimulated with reference compounds as shown in the figure. Following stimulation, calcium mobilization was detected using the DiscoverX’s HitHunter Calcium No WashPLUS detection kit (Cat. No. 90-0091) and IC50 was determined.

Inhibition of Cyclooxygenase COX2 by Reference Compounds

COX2 SAFETYscan Image

COX2 enzyme activity was determined by measuring the conversion of arachidonic acid to PPG2 based on fluorometirc readout. COX enzyme was incubated with the compounds at room temperature for 30 minutes before addition of the arachidonic acid (1.7 uM) and Ampliflu Red (2.5 uM).   Plate was read on a fluorimeter with the emission detection at 590 nm with excitation wavelength 544 nm.