| Assay ID | Title | Year | Journal | Article |
|---|
| AID1506676 | Antagonist activity at of C5aR in in human macrophages assessed as half life of residence time for maintaining reduction in C5a-induced macrophage response | | | |
| AID270448 | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID491628 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Selective hexapeptide agonists and antagonists for human complement C3a receptor. |
| AID491624 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release at 1 mM | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Selective hexapeptide agonists and antagonists for human complement C3a receptor. |
| AID1393266 | Antagonist activity at C5aR1 in human PMN | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID44471 | Antagonist activity against the C5a receptor | 2002 | Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
| Inhibition of protein-protein association by small molecules: approaches and progress. |
| AID270452 | Inhibition of C5a binding to human C5aR expressed in HEK293 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID270459 | Selectivity for C5aR over NK2 receptor | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID270455 | Binding affinity to NK2 receptor | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID270453 | Stability in human plasma after 1 hr at 37 degC | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID270456 | Binding affinity to MC4 receptor | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID1393269 | Oral bioavailability in Wistar rat at 10 mg/kg | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID270460 | Inhibition of C5a-induced chemotaxis of mouse J774A.1 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID491625 | Displacement of [125I-C3a] from C3a receptor in human PBMC at 1 mM by scintillation counting | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Selective hexapeptide agonists and antagonists for human complement C3a receptor. |
| AID1582631 | Antagonist activity at C5a receptor in human MDM cells assessed as inhibition of C5a-induced intracellular calcium release preincubated for 30 mins followed by C5a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
| Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity. |
| AID160504 | Antagonistic potency in the presence of 100 nM C5a measured by myeloperoxidase release from cytochalasin B stimulated human polymorphonuclear cells. | 2002 | Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
| Inhibition of protein-protein association by small molecules: approaches and progress. |
| AID270451 | Antagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase release | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID1393270 | Half life in Wistar rat at 10 mg/kg, po or 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID270454 | Inhibition of CYP3A4 at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID270458 | Binding affinity to V1a receptor | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID1393267 | Antagonist activity at C5aR1 in HMDM | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID270449 | Stability in human liver microsome after 1 hr | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID270457 | Binding affinity to ORL1 receptor | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
| AID1347000 | Human C5a1 receptor (Complement peptide receptors) | 2001 | Inflammation, Jun, Volume: 25, Issue:3
| Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes. |
| AID1347000 | Human C5a1 receptor (Complement peptide receptors) | 2004 | Molecular pharmacology, Apr, Volume: 65, Issue:4
| Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |