in vitro Assays & Screening List

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#ReceptorRadioligandReference Ligand
RBA047Adenosine A1[3H] DPCPXDPCPX
RBA007Adenosine A2A[3H] CGS 21680NECA
RBA091Adenosine A2A[3H] ZM-241385NECA
RBA048Adenosine A2B[3H] CPXNECA
RBA049Adenosine A3[125I] AB-MECAIB-MECA
RBA081Adenosine Trasnsporter[3H] NBTINBTI
RBA051Adrenergic a1[3H] PrazosinPrazosin
RBA008Adrenergic a1A[3H] PrazosinWB 4101
RBA009Adrenergic a1B[3H] PrazosinPhentolamine
RBA052Adrenergic a1D[3H] PrazosinPhentolamine
RBA053Adrenergic a2[3H] RX 821002RX 821002
RBA054Adrenergic a2A[3H] RX 821002RX 821002
RBA080Adrenergic a2C[3H] RX 821002RX 821002
RBA055Adrenergic ß[3H] DihydroalprenololPropranolol
RBA056Adrenergic ß1[3H] CGP 12177Alprenolol
RBA093Adrenergic ß1[125I] PindololAlprenolol
RBA057Adrenergic ß2[3H] CGP 12177Alprenolol
RBA092Adrenergic ß3[3H] CGP 12177Alprenolol
RBA058Adrenergic ß3[125I] PindololAlprenolol
RBA010Angiotensin II AT1[125I] Angiotensin IICandesartan
RBA011Angiotensin II AT2[125I] Angiotensin IIPD-123319
RBA084Bradykinin BK2[3H] BradykininBradykinin
RBA012Cannabinoid CB1[3H] SR 141716AWIN-55212-2
RBA094Cannabinoid CB1[3H] CP-55940CP-55940
RBA059Cannabinoid CB2[3H] A836339WIN-55212-2
RBA095Cannabinoid CB2[3H] CP-55940CP-55940
RBA085Cholecystokinin CCK1 (CCKA)[125I] CCK-8L-364718
RBA086Cholecystokinin CCK2 (CCKB)[125I] CCK-8Sincalide
RBA088Corticotropin Releasing Factor CRF1[125I] (Tyr0)-CRFUrocortin
RBA013Dopamine Transporter (DAT)[3H] WIN 35428WIN 35428
RBA014Dopamine D1[3H] SCH 23390SCH 23390
RBA015Dopamine D2[3H] RacloprideHaloperidol
RBA016Dopamine D2L[3H] methyl-spiperoneHaloperidol
RBA035Dopamine D3[3H] methyl-spiperoneHaloperidol
RBA036Dopamine D4[3H] methyl-spiperoneHaloperidol
RBA036Dopamine D4[3H] methyl-spiperoneHaloperidol
RBA037Dopamine D5[3H] SCH 23390SKF38393
RBA017GABAA[3H] MuscimolGABA
RBA018GABAA/BZP[3H] FlumazenilSKF38393
RBA032GABAB[3H] CGP 54626CGP 52432
RBA033Ca2+[3H] NitrendipineNifendipine
RBA034Na+ Site II[3H] BatrachotoxininVeratridine
RBA065Histamine H1[3H] PyrilaminePyrilamine
RBA066Histamine H2[3H] APTTiotidine
RBA067Histamine H3[3H] a-Me-Histaminea-Me-Histamine
RBA040mGluR2[3H] LY-341495MK801
RBA068Muscarinic M Non-Selective[3H] QNBAtropine
RBA069Muscarinic M1[3H] QNBAtropine
RBA070Muscarinic M2[3H] QNBAtropine
RBA071Muscarinic M3[3H] QNBAtropine
RBA072Muscarinic M4[3H] QNBAtropine
RBA073Muscarinic M5[3H] QNBAtropine
RBA019NDMA Ionotropic Gulatamate[3H] MK801MK801
RBA042 Norepinephrine Transporter (NET)[3H] NisoxetineDesipramine,
RBA024Nociceptin (ORL)[3H] NociceptinNociceptin
RBA020Opioid Non-Selective[3H] DiprenorphinDiprenorphine
RBA021Opioid DOR (δ)[125I ]Deltorphin IINaloxone
RBA022Opioid MOR (μ)[3H] DAMGONaloxone
RBA023Opioid KOR (κ)[3H] U69593Naloxone
RBA038Orexin Non-Selective[125I] Orexin-AOrexin-A
RBA028Orexin Non-Selective[3H] AlmorexantOrexin-A
RBA029Orexin 1 (OX1)[3H] SB 674042SB 334867
RBA030Orexin 2 (OX2)[3H] EMPAEMPA
RBA061Oxytocin[3H] OxytocinOxytocin
RBA025 Platelet-Activating Factor (PAF)[3H] PAFWEB 2086
RBA031Sigma (s) Non-Selective[3H] DTGHaloperidol
RBA026Sigma s1[3H] PentazocineHaloperidol
RBA027Sigma s2[3H] DTGHaloperidol
RBA062 Vasopressin1A[3H] AVPAVP
RBA063 Vasopressin1B[3H] AVPAVP
RBA064 Vasopressin2[3H] AVPAVP
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.