Find a Product

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 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
  • Better confidence using human target assays versus rodent orthologs
  • Functional data to support SAR analysis in lead optimization
  • Cost effective alternative to in house assay development and profiling

Learn more about SAFETYscan Ion Channel Services.

Safety44™ panel of  functional assays with all human targets for safety screening – Available Now

FamilyGene SymbolTargetReadout
AdrenoceptorsADRA2Aα2A-adrenoceptorcAMP formation
AdrenoceptorsADRB1β1-adrenoreceptorcAMP formation
AdrenoceptorsADRB2β2-adrenoreceptorcAMP formation
CannabinoidCNR1CB1cAMP formation
CannabinoidCNR2CB2cAMP formation
CholecystokininCCKARCCK1Calcium mobilization
DopamineDRD1D1cAMP formation
DopamineDRD2SD2ScAMP formation
EndothelinEDNRAETACalcium mobilization
HistamineHRH1H1Calcium mobilization
HistamineHRH2H2cAMP formation
AcetylcholineCHRM1M1Calcium mobilization
AcetylcholineCHRM2M2cAMP formation
AcetylcholineCHRM3M3Calcium mobilization
OpioidOPRD1δ-opioid receptorcAMP formation
OpioidOPRK1κ-opioid receptorcAMP formation
OpioidOPRM1μ-opioid receptorcAMP formation
5-HydroxytryptamineHTR1A5HT1AcAMP formation
5-HydroxytryptamineHTR1B5HT1BcAMP formation
5-HydroxytryptamineHTR2A5HT2ACalcium mobilization
5-HydroxytryptamineHTR2B5HT2BCalcium mobilization
Vasopressin and OxytocinAVPR1AV1ACalcium mobilization
AdenosineADORA2AA2ACalcium mobilization
AdenosineADRA1Aα1A-adrenoceptorCalcium mobilization
GABA receptorGABRA1GABAAMembrane potential
Serotonin receptorHTR3A5-HT-3Membrane potential
Calcium channelCACNA1CCAV1.2Calcium mobilization
Potassium channelKCNH2hERGPotassium channel activity
Sodium channelSCN5ANAV1.5Membrane potential
CyclooxygenaseCOX2COX2Enzymatic activity
CholinesteraseAChEAChEEnzymatic activity
Monoamine oxidaseMAOAMAOAEnzymatic activity
PhosphodiesterasePDE3APDE3AEnzymatic activity
PhosphodiesterasePDE4D2PDE4D2Enzymatic Activity
CyclooxygenaseCOX1COX1Enzymatic activity
NHRARARNuclear translocation
NHRGRGRNuclear translocation
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.