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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
FamilyTarget NameSpecies
Protein Kinase - radiometric enzyme assay
AGCPKAhuman
PKBβhuman
PKCmhuman
PKCzhuman
PKCαhuman
PKCβIhuman
PKCβIIhuman
PKCγhuman
PKCδhuman
PKCεhuman
PKCηhuman
PKCθhuman
PKCιhuman
PKG1ßhuman
PKG1αhuman
ROCK-IIhuman
CAMKAMPKrat
CaMKII βhuman
CaMKII γhuman
CaMKII δhuman
LKB1human
CMGCCDK1/cyclinBhuman
CDK2/cyclinAhuman
CDK2/cyclinEhuman
CDK3/cyclinEhuman
CDK5/p25human
CDK5/p35human
CDK7/cyclinH/MAT1human
CDK9/cyclinT1 human
GSK3b human
MAPK1human
MAPK2human
p70 S6 Kinasehuman
SAPK2ahuman
MiscPhKγ2human
TKAblhuman
Flt3human
IRhuman
Lynhuman


Protein Phosphatase - fluorescent enzyme assay
Tyrosine phosphatasePTP1Bhuman
TCPTPhuman


Ion Channel - cellular electrophysiology assay
Voltage-gated sodium channelNav1.5human
Inactivating potassium channelhKv4.3/hKChIP2human
Voltage-gated calcium channelL-type Calcium (Cav1.2)human
Ultra-rapid potassium channelhKv1.5human
Slow potassium channelhKCNQ1/hminKhuman
Rapid potassium channelhERGhuman
Hyperpolarization gated channel
hHCN4
hKir2.1
human
human
FamilyTarget NameSpecies
GPCR - cellular calcium flux assay
Acetylcholine (muscarinic)M1human
M2human
M3human
AdenosineA1human
A3human
Adrenergicalpha1Ahuman
alpha1Dhuman
alpha2Ahuman
beta 1human
beta 2human
AnaphylotoxinC5aRhuman
AngiotensinAT1human
BombesinBB2human
BradykininB2human
CalcitoninCGPR1human
CannabinoidCB1human
CB2human
ChemokineCCR1human
CCR2Bhuman
CX3CR1human
CXCR1human
CholecystokininCCK2human
CRF ReceptorCRF1human
DopamineD1human
D2Lhuman
D5human
EndothelinETAhuman
ETBhuman
GalaninGAL1human
Glycoprotein hormoneTSHhuman
GnRHGnRH / LHRHhuman
Histamine H1human
H2human
H3human
LeukotrieneBLT1human
CysLT1human
LysophospholipidLPA1human
LPA3human
S1P3human
MelanocortinMC5human
MotilinMotilin receptor, MTLRhuman
Neuromedin UNMU1human
Neuropeptide YY2human
NeurotensinNTR1human
N-formylpeptideFPR1human
Nicotinic AcidGPR109Ahuman
OpioidDeltahuman
Kappahuman
Muhuman
OrexinOX1human
OxytocinOThuman
P2Y / Purinergic (metabotropic)P2Y1human
Platelet Activating FactorPAFhuman
ProkineticinPK1human
Prolactin-releasing peptidePRPhuman
ProstanoidDPhuman
EP2human
EP3human
FPhuman
IP1human
TPhuman
Protease-activatedPAR4human
PTH receptorPTH1human
Serotonin5-HT1Ahuman
5-HT2Ahuman
5-HT2Bhuman
5-HT2Chuman
SomatostatinSST4human
Tackykinin /neurokininNK1human
NK3human
Urotensin IIUT / GPR14human
VasopressinV1Ahuman
V2human
VIP/PACAPPAC1 long isoformhuman
VPAC1human
VPAC2human