| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID747739 | Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125). |
| AID1065573 | Inhibition of N-terminal His-tagged Aurora A (unknown origin) using 5FAM-LRRASLG-CONH2 as substrate after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
| AID607712 | Inhibition of mitosis in human U2OS cells assessed as histone H3 phosphorylation at Ser 10 residue after 2 hrs by immunoassay | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607711 | Solubility of the compound at pH 7 | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID1065575 | Inhibition of full length CDK2/Cyclin A (unknown origin) using 5FAMQSPKKG-CONH2 as substrate after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
| AID607710 | Antiproliferative activity in human A2780 cells after 72 hrs by CellTiter-Glo assay | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607717 | Half life in mouse at 10 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607713 | Half life in mouse at 10 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607720 | Oral bioavailability in mouse at 10 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607718 | Cmax in mouse at 10 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607706 | Inhibition of MPS1 assessed as [33P]-gamma-ATP incorporation into substrate P38-betatide by gamma counting | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607715 | AUC in mouse at 10 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID747744 | Inhibition of MPS1 (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125). |
| AID1552053 | Inhibition of MPS1 (unknown origin) | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective. |
| AID607707 | Inhibition of Aur-A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607709 | Inhibition of PLK1 assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID1065579 | Growth inhibition in human HCT116 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
| AID607716 | Volume of distribution at steady state in mouse at 10 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607708 | Inhibition of CDK2/Cyclin A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID1552057 | Antitumor activity against human A2780 cells xenografted in mouse assessed as tumor growth inhibition at 90 mg/kg, po daily administered for 7 consecutive days relative to control | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective. |
| AID1065578 | Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
| AID607719 | AUC in mouse at 10 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607714 | Clearance in mouse at 10 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607721 | Antitumor activity against human A2780 cells xenografted in mouse assessed as tumor growth inhibition at 90 mg/kg, po for seven consecutive days | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID607722 | Toxicity in mouse assessed as body weight loss at at 90 mg/kg, po for seven consecutive days | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| AID1552055 | Half life in mouse xenografted with human A2780 cells at 90 mg/kg, po daily administered for 7 consecutive days | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective. |
| AID1065576 | Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
| AID1552056 | Oral bioavailability in mouse xenografted with human A2780 cells at 90 mg/kg daily administered for 7 consecutive days | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective. |
| AID1345801 | Human TTK protein kinase (TTK family) | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
| Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |