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Table 2 GPCR counterscreens of SCH 546738

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

Assay Inhibition (%) Assay Inhibition (%)
Adenosine A1 0% @ 4 μM Muscarinic M1 22% @ 4 μM
Adenosine A2A 3% @ 4 μM Muscarinic M2 52% @ 4 μM
Adrenergic α1A 11% @ 2 μM Muscarinic M3 27% @ 4 μM
Adrenergic α1B 25% @ 2 μM Muscarinic M4 30% @ 4 μM
Adrenergic α2A 45% @ 1 μM Muscarinic M5 28% @ 4 μM
Adrenergic α2B -2% @ 2 μM Neurokinin NK1 15% @ 2 μM
Adrenergic α2C 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 D4.2 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 5HT1A 20% @ 4 μM
MRGX1 1% @ 4 μM Vasopressin (V1a) 7% @ 4 μM
MRGX2 25% @ 4 μM Vasopressin (V1b) 15% @ 4 μM
   Vasopressin (V2) 18% @ 4 μM
   Vasopressin (oxytocin) 12% @ 4 μM
   VR1N 0% @ 4 μM
  1. SCH 546738 was tested at the indicated concentrations in a variety of GPCR assays according to established protocols.