Potency assay (off target):
The selectivity of JNJ-31020028 was
evaluated in a large variety of ion channels, transporters,
receptor binding, and kinase assays. These assays were
performed by CEREP and
Millipore, respectively.
Probe Selectivity in
Vitro:
JNJ-31020028 was assayed by binding in a panel of 50
receptors, ion channels, and transporters assays including
adenosine (A1, A2A, A3), adrenergic (α1, α2, β1), angioten-
sin (AT1), dopamine (D1, D2), bradykinin (B2), cholecysto-
kinin (CCKA), galanin (GAL 2 ), melatonin (ML 1 ),
muscarinic (M1, M2, M3), neurotensin (NT1), neurokinin
(NK2, NK3), opiate (μ, κ, δ), serotonin (5-HT1A, 5-HT1B,
5-HT 2A , 5-HT 3 , 5-HT 5A , 5-HT 6 , 5-HT 7 ), somatostatin,
vasopressin (V 1a), norepinephrine transporter, dopamine
transporter, and ion channels (sodium, calcium, potassium,
and chloride). The Y2 antagonist at concentrations up to
10μM had no significant affinity for any receptor/transport-
er/ion channel (<50% inhibition at 10μM) other than the Y2
receptor. Selectivity of Y2 antagonist was further evaluated
in a panel comprised of 65 kinases. JNJ-31020028 (10μM)
did not inhibit any of the kinase included in the panel
