Specializing in both standard and custom in vitro assays, we are focused on providing the right assays for target identification & validation, assay development, screening, hit-to-lead validation to help identify candidate compounds for preclinical and clinical development.

Below is a complete list of available assays.

Ref#ReceptorRadioligandReferenceSource
RBA047Adenosine A1[3H]DPCPXDPCPXT & C
RBA007Adenosine A2A[3H]CGS 21680NECAT & C
RBA091Adenosine A2A[3H]ZM-241385NECAT & C
RBA048Adenosine A2B[3H]CPXNECAC
RBA049Adenosine A3[125I]AB-MECAIB-MECAC
RBA081Adenosine Trasnsporter[3H]NBTINBTIC
RBA051Adrenergic a1[3H]PrazosinPrazosinT
RBA008Adrenergic a1A[3H]PrazosinWB 4101T & C
RBA009Adrenergic a1B[3H]PrazosinPhentolamineT & C
RBA052Adrenergic a1D[3H]PrazosinPhentolamineC
RBA053Adrenergic a2[3H]RX 821002RX 821002T
RBA054Adrenergic a2A[3H]RX 821002RX 821002C
RBA080Adrenergic a2C[3H]RX 821002RX 821002C
RBA055Adrenergic ß[3H]DihydroalprenololPropranololT
RBA056Adrenergic ß1[3H]CGP 12177AlprenololC
RBA093Adrenergic ß1[125I]PindololAlprenololC
RBA057Adrenergic ß2[3H]CGP 12177AlprenololC
RBA092Adrenergic ß3[3H]CGP 12177AlprenololC
RBA058Adrenergic ß3[125I]PindololAlprenololC
RBA010Angiotensin II AT1[125I]Angiotensin IICandesartanT & C
RBA011Angiotensin II AT2[125I]Angiotensin IIPD-123319T
RBA084Bradykinin BK2[3H]BradykininBradykininC
RBA012Cannabinoid CB1[3H]SR 141716AWIN-55212-2T & C
RBA094Cannabinoid CB1[3H]CP-55940CP-55940T & C
RBA059Cannabinoid CB2[3H]A836339WIN-55212-2C
RBA095Cannabinoid CB1[3H]CP-55940CP-55940C
RBA085Cholecystokinin CCK1 (CCKA)[125I]CCK-8L-364718C
RBA086Cholecystokinin CCK2 (CCKB)[125I]CCK-8SincalideC
RBA088Corticotropin Releasing Factor CRF1[125I](Tyr0)-CRFUrocortinC
RBA013Dopamine Transporter (DAT)[3H]WIN 35428WIN 35428T & C
RBA014Dopamine D1[3H]SCH 23390SCH 23390T & C
RBA015Dopamine D2[3H]RacloprideHaloperidolT & C
RBA016Dopamine D2L[3H]methyl-spiperoneHaloperidolC
RBA035Dopamine D3[3H]methyl-spiperoneHaloperidolC
RBA036Dopamine D4[3H]methyl-spiperoneHaloperidolC
RBA037Dopamine D5[3H]SCH 23390SKF38393C
RBA082Endothelin ETA[125I]Endothelin-1Endothelin-1C
RBA083Endothelin ETB[125I]Endothelin-1Endothelin-1C
RBA087Estrogen Receptor Non-selective[3H]Estradiol17ß-EstradiolC
RBA017GABAA[3H]MuscimolGABAT
RBA018GABAA/BZP[3H]FlumazenilFlumazenilT
RBA101GABAA/BZP[3H]FlunitrazepamFlumazenilT
RBA032GABAB[3H]CGP 54626CGP 52432T
RBA102GABAPBR[3H]-PK11195Ro5-4864T
RBA089GABA Transporter[3H]GABANO-711T
RBA090Glutamate AMPA[3H]AMPAL-Glutamic acidT
RBA019Glatamate NMDA[3H]MK801MK801T
RBA098HCA2[3H]NiacinNiacinC
RBA065Histamine H1[3H]PyrilamineChlorpheniramineC
RBA066Histamine H2[3H]APTTiotidineC
RBA096Histamine H2[125I]Iodo-aminopotentidineORG-5222C
RBA067Histamine H3[3H]a-Me-Histaminea-Me-HistamineC
RBA097Histamine H4[3H]-HistamineClozapineC
RBA075Imidazoline I2[3H]BU99008IdazoxanT
RBA033Ion Channel Ca2+[3H]NitrendipineNifendipineT
RBA034Ion Channel Na+ Site II[3H]BatrachotoxininVeratridineT
RBA060LRRK2[3H]LRRK2-IN-1LRRK2-IN-1T
RBA076LRRK2[3H]GNE-9605LRRK2-IN-1T
RBA078MAO-A[3H]HarmineClorgylineT
RBA079MAO-A[3H]Ro-41-1049ClorgylineT
RBA040mGluR2[3H]LY-341495MK801C
RBA041mGluR5[3H]M-MTEPMTEPT & C
RBA068Muscarinic M Non-Selectivce[3H]QNBAtropineT
RBA069Muscarinic M1[3H]QNBAtropineC
RBA070Muscarinic M2[3H]QNBAtropineT & C
RBA071Muscarinic M3[3H]QNBAtropineC
RBA072Muscarinic M4[3H]QNBAtropineC
RBA073Muscarinic M5[3H]QNBAtropineC
RBA042Norepinephrine Transporter (NET)[3H]NisoxetineDesipramineT & C
RBA024Nociceptin (ORL)[3H]NociceptinNociceptinC
RBA020Opioid Non-Selectivce[3H]DiprenorphinDiprenorphineT
RBA021Opioid DOR (δ)[125I]Deltorphin IINaloxoneC
RBA022Opioid MOR (µ)[3H]DAMGONaloxoneT & C
RBA023Opioid KOR (κ)[3H]U69593NaloxoneC
RBA074Orexin Non-Selective[125I]Orexin-AOrexin-AT
RBA028Orexin Non-Selective[3H]AlmorexantOrexin-AT
RBA029Orexin 1 (OX1)[3H]SB674042SB 334867C
RBA030Orexin 2 (OX2)[3H]EMPAEMPAC
RBA061Oxytocin[3H]OxytocinOxytocinC
RBA025Platelet-Activating Factor (PAF)[3H]PAFWEB 2086C
RBA044Serotonin 5-HT1[3H]SerotoninSerotoninT
RBA001Serotonin 5-HT1A[3H]WAY 1006358-OH-DPATC
RBA002Serotonin 5-HT1B[3H]AZ 10519369ErgotamineT
RBA003Serotonin 5-HT1B[3H]GR 125743ErgotamineT
RBA004Serotonin 5-HT1D[3H]GR 125743ErgotamineC
RBA045Serotonin 5-HT2[3H]KetanserinKetanserinT
RBA005Serotonin 5-HT2A[3H]MDL 100.907ChlorpromazineC
RBA038Serotonin 5-HT2B[3H]MesulergineSB 206553C
RBA039Serotonin 5-HT2B[125I]DOIDOIC
RBA050Serotonin 5-HT2C[3H]MesulegineMianserinC
RBA043Serotonin 5-HT3[3H]TropisetronMDL 72222C
RBA077Serotonin 5-HT6[3H]SB258585SerotoninC
RBA006Serotonin Transporter (SERT)[3H]ParoxetineFluoxetineT
RBA103Synaptic Vesivle Protein 2A (SV2A)[3H]UCB-JKeppraT & C
RBA031Sigma (σ) Non-Selective[3H]DTGHaloperidolT
RBA026Sigma σ1[3H]PentazocineHaloperidolT
RBA027Sigma σ2[3H]DTGHaloperidolC
RBA100Smoothened (SMO)[3H]CyclopamineSAGC
RBA099Sphingosine-1 Phosphate[3H]SphingosineS1PC
RBA062Vasopressin V1A[3H]AVPAVPC
RBA063Vasopressin V1B[3H]AVPAVPC
RBA064Vasopressin V2[3H]AVPAVPC
Primary & Secondary Radioligand Binding Assays

Compounds are typically subjected to primary radioligand binding assays at targets (receptors) selected by investigators. In the primary binding assays, compounds are usually tested at single concentrations (10 μM) in quadruplicate in 96-well plates. Compounds that show a minimum of 50% inhibition at 10 μM are tagged for secondary radioligand binding assays to determine equilibrium binding affinity at specific targets.

In the secondary binding assays, selected compounds are usually tested at 11 concentrations (0.1, 0.3, 1, 3, 10, 30, 100, 300 nM, 1, 3, 10 μM) and in triplicate.

Both primary and secondary radioligand binding assays are carried out in a final of volume of 125 μl per well in appropriate binding buffer. The hot ligand concentration is usually at a concentration close to the Kd (unless stated otherwise). Total and nonspecific binding are determined in the absence and presence of 10 μM of the appropriate reference compound, respectively. In brief, plates are incubated at a specific temperature in the dark for a specific amount of time (receptor specific). Reactions are stopped by vacuum filtration onto 0.3% polyethyleneimine (PEI) soaked 96-well Unifilters using a Filtermate harvester, followed by a wash with cold wash buffer. Scintillation cocktail is then added onto air-dried filters. Radioactivity is counted in a Microbeta counter.

Key details of our binding assay services:
  • Gold standard filtration assays.
  • Over 100 targets covered.
  • Single concentration screening or dose-response for IC50 determinations.
  • Percent inhibition (mean of replicates).
  • Individual values as a percent of control, IC50 value (calculated from a minimum of 6 concentration testing).
  • Quick turnaround times of 1-3 weeks depending on project types.
  • Plotted IC50 curves.
  • Proven skills and expertise to develop difficult targets.
  • Reliable, quick turnaround times.
  • High quality data with strict quality controls.
  • Flexible custom services to supplement our off-the-shelf services to meet your needs, providing a cost-effective way to expand your capabilities and capacity.