Assay ID | Title | Year | Journal | Article |
AID665635 | Volume of distribution at steady state in mouse at 2 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665601 | Fraction unbound in rat plasma | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665611 | Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665623 | Oral bioavailability in mouse at 10 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665633 | Volume of distribution at steady state in dog at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665626 | Half life in monkey at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665602 | Displacement of [125I]CGRP from CGRP receptor in dog brain membrane after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665638 | Displacement of [125I]adrenomedullin from human AM1 receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665631 | Clearance in mouse at 2 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665617 | Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins relative to control | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665622 | Oral bioavailability in monkey at 20 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665616 | Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serum | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665606 | Fraction unbound in monkey plasma | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665607 | Ratio of compound to MK-3207 fraction unbound in rat plasma | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665615 | Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serum | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665624 | Half life in rat at 2 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665621 | Oral bioavailability in monkey at 2 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665636 | Displacement of [125I]amylin from human AMY1 receptor expressed in COS7 cells after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665619 | Oral bioavailability in rat at 50 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665625 | Half life in dog at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665614 | Displacement of [125I]CGRP from mouse CGRP receptor | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665600 | Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665634 | Volume of distribution at steady state in monkey at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665618 | Oral bioavailability in rat at 5 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665645 | Ratio of compound to MK-3207 clearance in rat | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665610 | Aqueous solubility of the compound in citrate buffer at pH 2 | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665639 | Displacement of [125I]adrenomedullin from human AM2 receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665613 | Displacement of [125I]CGRP from rabbit CGRP receptor | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665632 | Volume of distribution at steady state in rat at 2 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665627 | Half life in mouse at 2 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665608 | Aqueous solubility of the compound in phosphate buffer at pH 7 | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665599 | Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665637 | Displacement of [125I]amylin from human AMY3 receptor expressed in COS7 cells after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665609 | Aqueous solubility of the compound in citrate buffer at pH 4 | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665603 | Antimigraine activity in iv dosed rat assessed as inhibition of capsaicin-induced dermal vasodilation administered 10 mins post capsaicin-challenge measured after 20 mins by laser doppler scanning | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665620 | Oral bioavailability in dog at 2 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665641 | Inhibition of Ikr ion channel by voltage clamp assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665629 | Clearance in dog at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665644 | Inhibition of CaV1.2 ion channel by voltage clamp assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665642 | Inhibition of Iks ion channel by voltage clamp assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665640 | Displacement of [125I]calcitonin from human CT receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665630 | Clearance in monkey at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665604 | Fraction unbound in human plasma | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665628 | Clearance in rat at 2 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665612 | Displacement of [125I]CGRP from CGRP receptor in rhesus monkey cerebellum after 3 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665643 | Inhibition of NaV1.5 ion channel by voltage clamp assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
AID665605 | Fraction unbound in dog plasma | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |