Ion Channel Screening & Profiling Services
IntroductionServices OverviewComprehensive Ion ChannelsCase Study
Brief Introduction
Ion channels are pore-forming membrane proteins that create a gated, water-filled pore to help establish and control voltage potential across cell membranes through control of the active flow of ions between the intracellular and the extracellular environments. As key components in a wide variety of biological processes involved in rapid changes in cells (e.g. cardiac/skeletal/smooth muscle contraction, and epithelial transport of nutrients), ion channels are important therapeutic targets in a range of indications, including cardiac, CNS, immune system and metabolic diseases. Due to the development of screening technologies, a dramatically increased interest has been shown in ion channels for hit validation, potency determination, selectivity profiling and lead optimization.
Figure. 1 The structure of ion channels.
Creative Biogene's Service Highlights
With over ten years in ion channel research, Creative Biogene understands client needs and works closely to reduce experimental risk, optimize assays, and deliver high-quality, reproducible data.
High-Throughput Ion Channel Screening
Creative Biogene's platforms allow rapid assessment of potency, efficacy, selectivity, and potential off-target effects. Both off-the-shelf and fully customized assays are available, covering major cardiac, CNS, and PNS channels. This approach enables early identification of promising leads while minimizing time and resource investment.
Flexible and Customizable Assays
Our ion channel services are designed to meet diverse project requirements, from high-throughput screening to lead optimization. Clients can select individual channels or design multi-channel panels tailored to their targets of interest. Customized assay conditions, including concentration ranges, stimulation protocols, and detection methods, can be incorporated to align with specific research goals.
Integrated Ion Channel Solutions
In addition to assay services, Creative Biogene offers a broad range of ion channel-related reagents and tools, including stable cell lines, premade viral particles, cell lysates, cloned constructs, and RNAi products. These resources provide a complete toolkit to support target validation, mechanistic studies, and preclinical development.
Broad-Spectrum Ion Channel Screening & Profiling
Ligand Gated Ion Channels
Creative Biogene provides a wide range of ligand-gated ion channels, including GABAA, P2X, nAChR, NMDA, and AMPA. Assays using manual patch clamp, Qpatch, FLIPR, and TEVC allow precise evaluation of activity, selectivity, and modulation, supporting hit identification and lead optimization.
| Channel | Official Symbol | Method |
| GABAA(α1β2γ2) | GABRA1/GABRB2/GABRG2 | Manual, Qpatch |
| GABAA(α1β3γ2) | GABRA1/GABRB3/GABRG2 | Manual |
| GABAA(α2β2γ2) | GABRA2/GABRB2/GABRG2 | Manual |
| GABAA(α2β3γ2) | GABRA2/GABRB3/GABRG2 | Manual |
| GABAA(α3β2γ2) | GABRA3/GABRB2/GABRG2 | Manual |
| GABAA(α3β3γ2) | GABRA3/GABRB3/GABRG2 | Manual |
| GABAA(α4β3γ2) | GABRA4/GABRB3/GABRG2 | Manual |
| GABAA(α4β3γ2) | GABRA4/GABRB3/GABRG2 | Manual |
| GABAA(α4β3δ) | GABRA4/GABRB3/GABRD | Manual |
| GABAA(α5β2γ2) | GABRA5/GABRB2/GABRG2 | Manual |
| GABAA(α5β3γ2) | GABRA5/GABRB3/GABRG2 | Manual |
| GABAA(α6β2γ2) | GABRA6/GABRB2/GABRG2 | Manual |
| GABAA(α6β3δ) | GABRA6/GABRB3/GABRD | Manual |
| Channel | Official Symbol | Method |
| hP2X1 | P2RX1 | Manual |
| hP2X3 | P2RX3 | Manual, Qpatch, FLIPR |
| rP2X3 | P2rx3 | Manual, FLIPR |
| gpP2X3 | P2rx3 | Manual |
| hP2X2/3 | P2RX2/P2RX3 | Manual, Qpatch, FLIPR |
| rP2X2/3 | P2rx2/P2rx3 | Manual, FLIPR |
| gpP2X2/3 | P2rx2/P2rx3 | Manual |
| hP2X4 | P2RX4 | Manual |
| hP2X5 | P2RX5 | Manual |
| hP2X7 | P2RX7 | Manual, FLIPR |
| Channel | Official Symbol | Method |
| nAChR-α3β4 | CHRNA3/CHRNB4 | TEVC bipolar |
| nAChR-α4β2 | CHRNA4/CHRNB2 | Manual, Qpatch, FLIPR |
| nAChR-α7/RIC3 | CHRNA7/αRIC3 | Manual, Qpatch, FLIPR |
| nAchRα1 | CHRNA1 | Activation or inhibition |
| nAchRα1 | CHRNA1 | Activation or inhibition, pre-incubation with nAch |
| nAChR-α7 | CHRNA7 | Activation or inhibition |
| nAChR-α7 | CHRNA7 | Activation or inhibition, pre-incubation with nAch |
| nAChR-α4β2 | CHRNA4/CHRNB2 | Activation or inhibition |
| nAChR-α4β2 | CHRNA4/CHRNB2 | Activation or inhibition, pre-incubation with nAch |
| nAChR(α1)2β1εδ | CHRNA1/CHRNB1/CHRNE/CHRND | Activation or inhibition |
| nAChR(α1)2β1εδ | CHRNA1/CHRNB1/CHRNE/CHRND | Activation or inhibition, pre-incubation with nAch |
| Channel | Official Symbol | Method |
| rNR1/NR2A | Grin1/Grin2a | Manual |
| hNR1/NR2A | GRIN1/GRIN2A | Manual |
| hNR1/NR2B | GRIN1/GRIN2B | Manual, TEVC bipolar |
| rNR1/NR2B | Grin1/Grin2b | Manual |
| hNR1/NR2C | GRIN1/GRIN2C | Manual |
| hNR1/NR2D | GRIN1/GRIN2D | Manual |
| Channel | Official Symbol | Method |
| AMPA | GRIA1 | Manual |
Voltage Gated Ion Channels (VGIC)
Our VGIC panel covers sodium, potassium, calcium channels, TRP, HCN, CRAC, and chloride channels. Flexible platforms enable single or multi-channel testing with customizable protocols, supporting HTS, lead optimization, and safety studies.
Sodium
Potassium
Calcium
TRP
HCN
Chloride
| Channel | Official Symbol | Method |
| NaV1.1 | SCN1A | Manual, Qpatch |
| NaV1.2 | SCN2A | Manual, Qpatch |
| NaV1.3 | SCN3A | Manual, Qpatch |
| NaV1.4 | SCN4A | Manual, Qpatch |
| NaV1.5 | SCN5A | Manual, Qpatch |
| NaV1.6 | SCN8A | Manual |
| NaV1.7 | SCN9A | Manual, Qpatch in optimization |
| rNaV1.7 | SCN9A | Manual |
| NaV1.8 | SCN10A | Manual |
| rNaV1.8 | SCN10A | Manual |
| Late Na | SCN5A | Manual |
| Channel | Official Symbol | Method |
| SK1 | KCNN1 | Manual |
| SK2 | KCNN2 | Manual |
| SK3 | KCNN3 | Manual |
| BKα1β1 | KCNMB1 | Manual |
| BKα1β4 | KCNMB4 | Manual |
| IK1/IKCa | KCNN4 | Manual |
| hERG/Kv11.1 | KCNH2 | Manual, Qpatch, FLIPR |
| KCNQ1/Kv7.1 | KCNQ1 /KCNE1 | Manual, Qpatch in optimization |
| KCNQ2/Kv7.2 | KCNQ2 | Manual |
| KCNQ3/Kv7.3 | KCNQ3 | Manual |
| KCNQ4/Kv7.4 | KCNQ4 | Manual |
| KCNQ5/Kv7.5 | KCNQ5 | Manual |
| KCNQ2/3 | KCNQ2/KCNQ3 | Manual, Qpatch |
| KCNQ2/4 | KCNQ2/KCNQ4 | Manual |
| KCNQ3/5 | KCNQ3/KCNQ5 | Manual |
| Kir2.1 | KCNJ2 | Manual |
| Kir3.1/3.4 | KCNJ3/KCNJ5 | Manual |
| Kir3.2 | KCNC2 | Manual |
| Kir4.1 | KCNJ10 | Qpatch to be optimized, FLIPR |
| Kir6.2/SUR2A | KCNJ11/ABCC9 | Manual |
| Kir6.2/SUR1 | KCNJ11/ABCC8 | Manual |
| TREK1 | KCNK2 | Manual |
| TASK1 | KCNK3 | Manual |
| TASK2 | KCNK5 | Manual |
| Kv1.1 | KCNA1 | Manual |
| Kv1.2 | KCNA2 | Manual |
| Kv1.3 | KCNA3 | Manual, Qpatch |
| Kv1.4 | KCNA4 | Manual |
| Kv1.5 | KCNA5 | Manual |
| Kv1.6 | KCNA6 | Manual |
| Kv1.7 | KCNA7 | Manual |
| Kv2.1 | KCNB1 | Manual |
| Kv2.2 | KCNB2 | Manual |
| Kv3.1 | KCNC1 | Manual |
| Kv3.2 | KCNC2 | Manual |
| Kv3.4 | KCNC4 | Manual |
| Kv4.2/KChIP2.2 | KCND2/KCNIP2 | Manual, Qpatch in optimization |
| Kv4.3 | KCND3 | Manual, Qpatch in optimization |
| Channel | Official Symbol | Method |
| CaV1.1 | CACNA1S/CACNB2/CACNA2D | Manual |
| CaV1.2 (L-type) | CACNA1C/CACNB2/CACNA2D1 | Manual, Qpatch in optimization |
| CaV1.3 | CACNA1D/CACNB3/CACNA2D | Manual |
| CaV1.4 | CACNA1F/CACNB2/CACNA2D | Manual |
| CaV2.1 (P/Q-type) | CACNA1A/CACNB4/CACNA2D1 | Manual |
| CaV2.2 (N-type) | CACNA1B/CACNB3/CACNA2D1 | Manual, Qpatch & FLIPR in optimization |
| CaV2.3 | CACNA1E/CACNB3/CACNA2D | Manual |
| CaV3.1 | CACNA1G | Manual |
| CaV3.2 (T-type) | CACNA1H | Manual |
| CaV3.3 | CACNA1I | Manual |
| CRAC (STIM1/Orai) | STIM1/Orai | Manual |
| Channel | Official Symbol | Method |
| TRPA1 | TRPA1 | Manual, FLIPR |
| TRPC1 | TRPC1 | Manual |
| TRPC5 | TRPC5 | Manual |
| TRPC6 | TRPC6 | Manual, FLIPR |
| TRPC7 | TRPC7 | Manual |
| TRPM3 | TRPM3 | Manual |
| TRPM4/SUR1 | TRPM4/ABCC8 | Manual |
| TRPM8 | TRPM8 | Manual, FLIPR |
| TRPML1 | TRPML1 | Manual |
| TRPML3 | TRPML3 | Manual |
| TRPV1 | TRPV1 | Manual, FLIPR |
| TRPV2 | TRPV2 | Manual |
| TRPV3 | TRPV3 | Manual |
| TRPV4 | TRPV4 | Manual, FLIPR |
| TPC2 | TPCN2 | Manual |
| Channel | Official Symbol | Method |
| HCN1 | HCN1 | Manual |
| HCN2 | HCN2 | Manual |
| HCN3 | HCN3 | Manual |
| HCN4 | HCN4 | Manual |
| Channel | Official Symbol | Method |
| CFTR | CFTR | Manual, TEVC bipolar |
| TMEM16A | ANO-1 | Manual |
| TMEM16B | ANO-2 | Manual |
| CLCN1 | CLCN1 | Manual |
Others
We also provide assays for other important channels, including 5-HT3A, ASICs, and GlyR. Multiple assay formats deliver reliable, reproducible data to accelerate target validation and screening.
| Channel | Official Symbol | Method |
| 5-HT3A | HTR3A | Manual, Qpatch, FLIPR, TEVC bipolar |
| ASIC1a | ASIC1 | Manual |
| ASIC1b | ASIC1 | Manual |
| ASIC3 | ASIC3 | Manual |
| GlyRα1/β | GLRA1/GLRB | Manual |
Case Study
The research team aimed to investigate the effects of a chemically modified α-cobratoxin (mToxin) on α7 nicotinic acetylcholine receptors (α7AChR). Using Creative Biogene's Ion Channel Screening & Profiling Services, PC12 cells expressing α7AChR were cultured and prepared for manual patch clamp recordings. Cells were seeded into 24-well plates with coverslips and incubated to reach appropriate confluency. The team applied mToxin and recorded receptor currents, generating quantitative data on its effects on α7AChR activity under controlled in vitro conditions.
Figure 2. Whole-cell patch-clamp recordings in PC12 cells showing that mToxin alone does not evoke currents but partially inhibits α7AChR-mediated responses induced by AR-R17779. (Fonar G, et al., 2021)
Contact Us
If you have any special requirements in ion channel compound screening, please feel free to contact us. We are looking forward to working together with your attractive projects.
References
- Bagal SK, Brown AD, Cox PJ, et al. Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624.
- Fonar G, Polis B, Sams DS, et al. Modified Snake α-Neurotoxin Averts β-Amyloid Binding to α7 Nicotinic Acetylcholine Receptor and Reverses Cognitive Deficits in Alzheimer's Disease Mice. Mol Neurobiol. 2021 May;58(5):2322-2341.
Publications
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Fonar G, Polis B, Sams D S, et al. Modified Snake α-Neurotoxin Averts β-Amyloid Binding to α7 Nicotinic Acetylcholine Receptor and Reverses Cognitive Deficits in Alzheimer’s Disease Mice[J]. Molecular neurobiology, 2021, 58: 2322-2341.
* For research use only. Not intended for any clinical use.