A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection

Table 2 GPCR counterscreens of SCH 546738

Assay	Inhibition (%)	Assay	Inhibition (%)
Adenosine A₁	0% @ 4 μM	Muscarinic M₁	22% @ 4 μM
Adenosine A_2A	3% @ 4 μM	Muscarinic M₂	52% @ 4 μM
Adrenergic α_1A	11% @ 2 μM	Muscarinic M₃	27% @ 4 μM
Adrenergic α_1B	25% @ 2 μM	Muscarinic M₄	30% @ 4 μM
Adrenergic α_2A	45% @ 1 μM	Muscarinic M₅	28% @ 4 μM
Adrenergic α_2B	-2% @ 2 μM	Neurokinin NK₁	15% @ 2 μM
Adrenergic α_2C	76% @ 1 μM	Neurokinin NK₂	0% @ 2 μM
CCR1	9% @ 10 μM	Neurokinin NK₃	0% @ 2 μM
CCR2	9% @ 10 μM	Neuropeptide Y (Y₁)	4% @ 4 μM
CCR3	17% @ 10 μM	Neuropeptide Y (Y₂)	-9% @ 4 μM
CCR5	10% @ 10 μM	Neuropeptide Y (Y₄)	-2% @ 4 μM
CCR7	0% @ 10 μM	Neuropeptide Y (Y₅)	12% @ 4 μM
CXCR1	13% @ 10 μM	Nociceptin NOP₁	-21% @ 4 μM
CXCR2	20% @ 10 μM	Delta opiate	12% @ 4 μM
Dopamine D₁	6% @ 4 μM	Kappa opiate	7% @ 4 μM
Dopamine D₂	41% @ 4 μM	Mu opiate	22% @ 4 μM
Dopamine D₃	18% @ 10 μM	Prokineticin PKR₁	-1% @ 4 μM
Dopamine D_4.2	18% @ 10 μM	Prokineticin PKR₂	-5% @ 4 μM
Histamine H₁	46% @ 2 μM	Purinergic P2Y₁	16% @ 4 μM
Histamine H₃	29% @ 2 μM	Purinergic P2Y1₂	10% @ 4 μM
MCHR₁	0% @ 10 μM	Serotonergic 5HT_1A	20% @ 4 μM
MRGX₁	1% @ 4 μM	Vasopressin (V_1a)	7% @ 4 μM
MRGX₂	25% @ 4 μM	Vasopressin (V_1b)	15% @ 4 μM
		Vasopressin (V₂)	18% @ 4 μM
		Vasopressin (oxytocin)	12% @ 4 μM
		VR1N	0% @ 4 μM

SCH 546738 was tested at the indicated concentrations in a variety of GPCR assays according to established protocols.

ISSN: 1471-2172