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

• 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

Get Started

• Log in to our Drug Discovery & Development Service Portal

View Our Service Portfolio

• Lead Discovery Target Panels

Targets Available in the Drug Discovery Safety & Liability Screening Panel

Family Target Name Species 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 Protein Phosphatase - fluorescent enzyme assay Tyrosine phosphatase PTP1B human TCPTP human Ion Channel - cellular electrophysiology assay 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

Family Target Name Species 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

flx_root