Lead Discovery - Safety & Liability Screening
BIRB0796 Inhibition of Cardiac Ion Channels
BIRB0796 was developed as a kinase inhibitor to treat chronic inflammation. Its development was halted during clinical trials due to reported hepatotoxicity. To investigate other potential off-target effects, this compound was assayed at 10 μM against cardiac ion channels included in the Safety & Liability Screening Panel. Results indicate significant inhibition of hERG and hKv1.5 currents, indicating potential cardiotoxicity.
Safety and Liability Screening Panel
Providing critical early assessment across a range of targets, our safety and toxicity service panel is more predictive and biologically relevant, empowering you to make better decisions.
The Safety & Liability Screening Panel provides industry-leading, functional profiling against 125 GPCR, kinase, ion channel and phosphatase targets. These targets were specifically chosen for their relevance to critical diseases and key pathways, including:
- Neurotoxicity
- Cardiac safety
Advantages of Millipore’s Safety and Liability Screening Services
- Recognized quality and service from our premier functional profiling services in one convenient service panel
- Single compound shipping point to your choice of the US or UK, reducing your shipping and administrative costs
- Convenient monthly schedule with three-week turnaround
- Valuable insight into potential off-target liabilities at an extraordinary value
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Targets Available in the Drug Discovery Safety & Liability Screening Panel
| Protein Kinase - radiometric enzyme assay |
| AGC | PKA | human |
 | PKBβ | human |
 | PKCm | human |
 | PKCz | human |
 | PKCα | human |
 | PKCβI | human |
 | PKCβII | human |
 | PKCγ | human |
 | PKCδ | human |
 | PKCε | human |
 | PKCη | human |
 | PKCθ | human |
 | PKCι | human |
 | PKG1ß | human |
 | PKG1α | human |
 | ROCK-II | human |
| CAMK | AMPK | rat |
 | CaMKII β | human |
 | CaMKII γ | human |
 | CaMKII δ | human |
 | LKB1 | human |
| CMGC | CDK1/cyclinB | human |
 | CDK2/cyclinA | human |
 | CDK2/cyclinE | human |
 | CDK3/cyclinE | human |
 | CDK5/p25 | human |
 | CDK5/p35 | human |
 | CDK7/cyclinH/MAT1 | human |
 | CDK9/cyclinT1 | human |
 | GSK3b | human |
 | MAPK1 | human |
 | MAPK2 | human |
 | p70 S6 Kinase | human |
 | SAPK2a | human |
| Misc | PhKγ2 | human |
| TK | Abl | human |
 | Flt3 | human |
 | IR | human |
| | Lyn | human |
| Tyrosine phosphatase | PTP1B | human |
| | TCPTP | human |
| Voltage-gated sodium channel | Nav1.5 | human |
| Inactivating potassium channel | hKv4.3/hKChIP2 | human |
| Voltage-gated calcium channel | L-type Calcium (Cav1.2) | human |
| Ultra-rapid potassium channel | hKv1.5 | human |
| Slow potassium channel | hKCNQ1/hminK | human |
| Rapid potassium channel | hERG | human |
Hyperpolarization gated channel
| hHCN4
hKir2.1 | human
human |
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| GPCR - cellular calcium flux assay |
| Acetylcholine (muscarinic) | M1 | human |
 | M2 | human |
 | M3 | human |
| Adenosine | A1 | human |
 | A3 | human |
| Adrenergic | alpha1A | human |
 | alpha1D | human |
 | alpha2A | human |
 | beta 1 | human |
 | beta 2 | human |
| Anaphylotoxin | C5aR | human |
| Angiotensin | AT1 | human |
| Bombesin | BB2 | human |
| Bradykinin | B2 | human |
| Calcitonin | CGPR1 | human |
| Cannabinoid | CB1 | human |
 | CB2 | human |
| Chemokine | CCR1 | human |
 | CCR2B | human |
 | CX3CR1 | human |
 | CXCR1 | human |
| Cholecystokinin | CCK2 | human |
| CRF Receptor | CRF1 | human |
| Dopamine | D1 | human |
 | D2L | human |
 | D5 | human |
| Endothelin | ETA | human |
 | ETB | human |
| Galanin | GAL1 | human |
| Glycoprotein hormone | TSH | human |
| GnRH | GnRH / LHRH | human |
| Histamine | H1 | human |
 | H2 | human |
 | H3 | human |
| Leukotriene | BLT1 | human |
 | CysLT1 | human |
| Lysophospholipid | LPA1 | human |
 | LPA3 | human |
 | S1P3 | human |
| Melanocortin | MC5 | human |
| Motilin | Motilin receptor, MTLR | human |
| Neuromedin U | NMU1 | human |
| Neuropeptide Y | Y2 | human |
| Neurotensin | NTR1 | human |
| N-formylpeptide | FPR1 | human |
| Nicotinic Acid | GPR109A | human |
| Opioid | Delta | human |
 | Kappa | human |
 | Mu | human |
| Orexin | OX1 | human |
| Oxytocin | OT | human |
| P2Y / Purinergic (metabotropic) | P2Y1 | human |
| Platelet Activating Factor | PAF | human |
| Prokineticin | PK1 | human |
| Prolactin-releasing peptide | PRP | human |
| Prostanoid | DP | human |
 | EP2 | human |
 | EP3 | human |
 | FP | human |
 | IP1 | human |
 | TP | human |
| Protease-activated | PAR4 | human |
| PTH receptor | PTH1 | human |
| Serotonin | 5-HT1A | human |
 | 5-HT2A | human |
 | 5-HT2B | human |
 | 5-HT2C | human |
| Somatostatin | SST4 | human |
| Tackykinin /neurokinin | NK1 | human |
 | NK3 | human |
| Urotensin II | UT / GPR14 | human |
| Vasopressin | V1A | human |
 | V2 | human |
| VIP/PACAP | PAC1 long isoform | human |
 | VPAC1 | human |
 | VPAC2 | human |
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