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up to 3 uM
1H NMR (400MHz, CD3OD) δ 7.98 (d, J = 6.2 Hz, 1H), 7.08 (d, J = 2.3 Hz, 2H), 6.68 (d, J = 2.6 Hz, 1H), 6.64 (dd, J = 6.3, 2.6 Hz, 1H), 6.61 (t, J = 2.3 Hz, 1H), 3.26 (ddd, J = 13.6, 10.7, 3.3 Hz, 2H), 2.87 – 2.83 (m, 2H), 2.38 (s, 3H), 2.38 (s, 3H), 1.98 (ddd, J = 14.8, 10.8, 4.6 Hz, 2H), 1.66 (dd, J = 13.9, 3.9 Hz, 2H)
Selectivity against 32 methyltransferases (MTs) were tested at 1 µM and 10 µM of compounds. PRDM9 was the only methyltransferase in a panel of MTs that was inhibited by MRK-740
MRK-740 was profiled in a customized panel of 108 enzymes and receptors at Eurofins Panlabs Discovery Services, Taiwan. MRK-740 demonstrated significant (>50% at 10 µM) binding only to Adrenergic α2B, Histamine H3, Muscarinic M2 and Opiate µ receptors. Functional assessment for these four GPCRs in agonist and antagonist mode revealed no functional activity on Adrenergic α2B, Histamine H3 & Muscarinic M2 receptors, and some potential agonistic activity at the Opiate µ receptor.
