Assay ID | Title | Year | Journal | Article |
AID539993 | Protein binding in human serum assessed as unbound fraction | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539989 | Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539997 | Inhibition of cynomolgus CCR2 | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539990 | Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539995 | Inhibition of human ERG | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540003 | Cmax in CD-1 mouse at 10 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540000 | Clearance in CD-1 mouse at 5 mg/kg, iv | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539992 | Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539991 | Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540002 | Half life in CD-1 mouse at 5 mg/kg, iv | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539994 | Protein binding in mouse serum assessed as unbound fraction | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540007 | AUC in BALB/c mouse at 10 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540006 | Cmax in BALB/c mouse at 10 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540001 | Volume of distribution at steady state in CD-1 mouse at 5 mg/kg, iv | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540004 | AUC in CD-1 mouse at 10 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539999 | Inhibition of mouse CCR5 | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539998 | Inhibition of mouse CCR1 | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID539996 | Inhibition of rat CCR2 | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID540005 | Oral bioavailability in CD-1 mouse at 10 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346744 | Mouse CCR2 (Chemokine receptors) | 2005 | Journal of immunology (Baltimore, Md. : 1950), Oct-15, Volume: 175, Issue:8
| Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344. |
AID771594 | Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes assessed as association and dissociation of radioligand | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
| Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. |
AID771595 | Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
| Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. |
AID771593 | Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes assessed as association and dissociation of compound by competition association assay | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
| Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. |
AID771596 | Displacement of [3H]INCB3344 from human CCR2 receptor expressed in human U2OS cell membranes by saturation binding assay | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
| Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |