Assay ID | Title | Year | Journal | Article |
AID706998 | Genotoxicity in Sprague-Dawley rat assessed as micronucleated polychromatic erythrocytes in bone marrow at 100 mg/kg, po qd for 2 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706993 | Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 100 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706994 | Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 50 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707004 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser1292 in ip dosed BAC transgenic mouse brain after 1 to 24 hrs | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706988 | Ratio of drug level CSF to unbound drug level in plasma in cynomolgus monkey at 10 to 65 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707015 | Inhibition of TTK at 0.1 uM | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706992 | Unbound plasma AUC (0 to 24 hrs) in cynomolgus monkey at 10 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707024 | Inhibition of autophosphorylation of LRRK2 in human HEK293 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707020 | Clearance in rat hepatocytes | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1821425 | Unbound brain-to-plasma concentration ratio in rat at 2.5 uM incubated for 4 hrs by equilibrium dialysis method | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
AID706990 | Ratio of unbound drug level in brain to plasma in cynomolgus monkey at 10 to 65 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1462813 | Inhibition of recombinant human wild type GST-tagged LRRK2 (970 to 2527 residues) preincubated for 30 mins followed by fluorescein-LRRKtide substrate addition after 2 hrs by TR-FRET assay | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors. |
AID707003 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser1292 in po dosed BAC transgenic mouse brain after 1 to 24 hrs | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707021 | Clearance in human hepatocytes | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707008 | Inhibition of LRRK2 using FAM-LRRKtide as substrate at 0.1 uM after 120 mins by microfluidic capillary electrophoresis assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707006 | Inhibition of recombinant human 5HT2B receptor expressed in CHO cells at 10 uM | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1821470 | Unbound brain-to-plasma concentration ratio in non-human primates administered orally and measured after 120 mins by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
AID706989 | Unbound plasma AUC (0 to 24 hrs) in cynomolgus monkey at 65 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706995 | Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706996 | Toxicity in Sprague-Dawley rat assessed as mortality at 10 to 100 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1821424 | Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human MDR1-transfected dog MDCKII-MDR1 cells at 0.1 to 1 uM measured after 3 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
AID707012 | Selectivity ratio of Ki for TTK to Ki for LRRK2 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707019 | Plasma protein binding in rat | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1071301 | Selectivity ratio of Ki for JAK2 (unknown origin) to Ki for LRRK2 (unknown origin) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707018 | Apparent permeability from apical to basolateral side of MDCK cells expressing human MDR1 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707000 | Clearance in cynomolgus monkey hepatocytes | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706991 | Unbound plasma AUC (0 to 24 hrs) in cynomolgus monkey at 25 mg/kg, po administered for 7 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707026 | Inhibition of LRRK2 using FAM-LRRKtide as substrate after 120 mins by microfluidic capillary electrophoresis assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707017 | Efflux ratio of permeability from apical to basolateral over basolateral to apical side in MDCK cells expressing human MDR1 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1673916 | Inhibition of LRRK2 G2019S mutant (unknown origin) | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
| Monomeric Targeted Protein Degraders. |
AID1462812 | Inhibition of recombinant human LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus preincubated for 30 mins followed by fluorescein-LRRKtide substrate addition after 2 hrs by TR-FRET assay | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors. |
AID706999 | Plasma protein binding in cynomolgus monkey | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707023 | Selectivity ratio of Ki for JAK2 to Ki for LRRK2 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1071302 | Thermodynamic solubility of the crystalline form of compound at pH 7.4 | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID707007 | Inhibition of ALK at 0.1 uM | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID706997 | Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 100 mg/kg, po qd for 2 days | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
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. |
AID1345801 | Human TTK protein kinase (TTK family) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
AID1345739 | Human leucine rich repeat kinase 2 (Leucine-rich repeat kinase (LRRK) family) | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |