| Assay ID | Title | Year | Journal | Article |
|---|
| AID1442513 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side in pig LLC-PK1 cells expressing human MDR1 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1880672 | Inhibition of full-length LRRK2 G2019S mutant (unknown origin) using LRRKtide as substrate incubated for 1 hr in presence of ATP by TR-FRET based ADAPTA assay | 2022 | ACS medicinal chemistry letters, Jun-09, Volume: 13, Issue:6
| Discovery of 1 |
| AID1442512 | Inhibition of recombinant human GST-tagged LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus using fluorescein-ERM as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by TR-FRET assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1673902 | Inhibition of recombinant human GST-tagged LRRK2 G2019S mutant catalytic domain (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr b | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
| Monomeric Targeted Protein Degraders. |
| AID1442517 | Intrinsic clearance in rat hepatocytes assessed per million cells at 1 uM after 180 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1900451 | Inhibition of pcDNA5FRT-TO-GFP fused - LRRK2 (unknown origin) transfected in HEK293 cells assessed as remaining activity at 30 uM incubated for 24 hrs by ELISA relative to control | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1442546 | In vivo inhibition of LRRK2 Ser935 phosphorylation in mouse brain assessed as unbound plasma concentration causing reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at 1 to 100 mg/kg, po administered 1 hr post treatment by Western blot an | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442533 | Inhibition of human CYP2D6 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1853292 | Brain to plasma permeability coefficient, Kp in CD rat plasma assessed as unbound fraction at 3 to 100 mg/kg, po and measured after 2 hrs by LC/MS/MS analysis | 2021 | RSC medicinal chemistry, Jul-21, Volume: 12, Issue:7
| Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors. |
| AID1442547 | Equilibrium solubility in Water after 24 hrs by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1821511 | In vivo inhibition of LRRK2 in CD rat assessed as reduction in phosphorylation at Ser935 residue in striatum at 10 mg/kg, po measured after 2 hrs by MSD assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
| AID1900450 | Inhibition of pcDNA5FRT-TO-GFP fused - LRRK2 G2019S mutant (unknown origin) transfected in HEK293 cells incubated for 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1442532 | Fraction unbound in rat plasma at 10 uM after 4 hrs by rapid equilibrium dialysis method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442550 | Equilibrium solubility in pH 6.5 Phosphate buffer after 24 hrs by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1900446 | Inhibition of full length wild type LRRK2 (unknown origin) by LRRKtide Adapta assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1442548 | Equilibrium solubility in simulated gastric fluid after 24 hrs by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442514 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side in pig LLC-PK1 cells expressing rat MDR1 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442540 | In vivo inhibition of LRRK2 Ser935 phosphorylation in CD rat brain cortex assessed as unbound brain concentration causing reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at 1 to 100 mg/kg, po administered 1 hr post treatment by Western | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1865942 | Inhibition of LRRK2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 56 | A survey of the clinical pipeline in neuroscience. |
| 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. |
| AID1442516 | Intrinsic clearance in human hepatocytes assessed per million cells at 1 uM after 180 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442522 | AUC (0 to 8 hrs) in Han-Wistar rat at 2 mg/kg, iv measured after 2 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442520 | Inhibition of recombinant human GST-tagged LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus using fluorescein-ERM as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr in presence of 5 mM ATP by TR-FRE | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1900455 | Inhibition of LRRK2 G2019S/A2016T double mutant (unknown origin) transfected in HEK293 cells upto 300 nM incubated for 24 hrs by immunoblotting method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1900453 | Inhibition of wild type LRRK2 (unknown origin) transfected in HEK293 cells upto 300 nM incubated for 24 hrs by immunoblotting method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1880674 | Inhibition of mouse full-length LRRK2 G2019S mutant transfected in HEK293 cells using LRRKtide as substrate in presence of ATP by incubated for 1 hr TR-FRET based ADAPTA assay | 2022 | ACS medicinal chemistry letters, Jun-09, Volume: 13, Issue:6
| Discovery of 1 |
| 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. |
| AID1442524 | Half life in Han-Wistar rat at 2 mg/kg, iv measured after 2 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442526 | Clearance in Han-Wistar rat at 2 mg/kg, iv measured after 2 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442528 | Cmax in Han-Wistar rat at 10 mg/kg, po measured after 15 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442531 | Oral bioavailability in Han-Wistar rat at 10 mg/kg, measured after 15 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| 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. |
| AID1442536 | Time dependent inhibition of human CYP3A4 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1900452 | Selectivity ratio of IC50 for wild type pcDNA5FRT-TO-GFP fused - LRRK2 (unknown origin) to IC50 for pcDNA5FRT-TO-GFP fused - LRRK2 G2019S mutant transfected in HEK293 cells | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1880673 | Selectivity ratio, ratio of IC50 for full-length wild type LRRK2 (unknown origin) to IC50 for full-length LRRK2 G2019S mutant (unknown origin) | 2022 | ACS medicinal chemistry letters, Jun-09, Volume: 13, Issue:6
| Discovery of 1 |
| AID1442552 | Equilibrium solubility in pH 5 acetate buffer after 24 hrs by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442539 | In vivo inhibition of LRRK2 Ser935 phosphorylation in po dosed CD rat brain cortex assessed as reduction in ratio of phosphorylated Ser935 to total LRRK2 protein administered 1 hr post treatment by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442529 | Tmax in Han-Wistar rat at 10 mg/kg, po measured after 15 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442538 | In vivo inhibition of LRRK2 Ser935 phosphorylation in CD rat brain cortex assessed as reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at => 30 mg/kg, po administered 1 hr post treatment by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442523 | Initial concentration in Han-Wistar rat at 2 mg/kg, iv measured after 2 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442534 | Inhibition of human CYP2C9 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442525 | MRT in Han-Wistar rat at 2 mg/kg, iv measured after 2 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1900447 | Inhibition of full length LRRK2 G2019S mutant (unknown origin) by LRRKtide Adapta assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1442521 | Inhibition LRRK2 G2019S mutant Ser935 phosphorylation in human SH-SY5Y cells after 90 mins by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1821476 | Unbound brain-to-plasma concentration ratio in CD rat 1 to 100 mg/kg, po 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. |
| AID1900454 | Inhibition of LRRK2 G2019S mutant (unknown origin) transfected in HEK293 cells upto 300 nM incubated for 24 hrs by immunoblotting method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1900449 | Inhibition of wild type pcDNA5FRT-TO-GFP fused - LRRK2 (unknown origin) transfected in HEK293 cells incubated for 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1442545 | In vivo inhibition of LRRK2 Ser935 phosphorylation in mouse brain assessed as unbound brain concentration causing reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at 1 to 100 mg/kg, po administered 1 hr post treatment by Western blot ana | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442537 | In vivo inhibition of LRRK2 Ser935 phosphorylation in mouse brain cortex assessed as reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at =>10 mg/kg, po administered 1 hr prior to euthanasia measured by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442551 | Equilibrium solubility in fed state simulated intestinal fluid after 24 hrs by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1880671 | Inhibition of full-length wild type LRRK2 (unknown origin) using LRRKtide as substrate incubated for 1 hr in presence of ATP by TR-FRET based ADAPTA assay | 2022 | ACS medicinal chemistry letters, Jun-09, Volume: 13, Issue:6
| Discovery of 1 |
| AID1442530 | MRT in Han-Wistar rat at 10 mg/kg, po measured after 15 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442535 | Inhibition of human CYP3A4 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1900448 | Selectivity ratio of IC50 for wild type LRRK2 (unknown origin) to IC50 for LRRK2 G2019S mutant (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy. |
| AID1442549 | Equilibrium solubility in fasted state simulated intestinal fluid after 24 hrs by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442515 | Apparent permeability in pig LLC-PK1 cells expressing human MDR1 | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442541 | In vivo inhibition of LRRK2 Ser935 phosphorylation in CD rat brain cortex assessed as unbound plasma concentration causing reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at 1 to 100 mg/kg, po administered 1 hr post treatment by Western | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1442544 | Ratio of IC50 in Inhibition of recombinant human GST-tagged LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus in presence of 5 mM ATP to IC50 for Inhibition of recombinant human GST-tagged LRRK2 (970 to 2527 residues) G2019S mutant expre | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| AID1853289 | Invivo inhibition of LRRK2 in CD rat assessed as reduction in serine 935 phosphorylated LRRK2 in striatum at 10 mg/kg, po and measured after 2 hrs by MSD immunoassay | 2021 | RSC medicinal chemistry, Jul-21, Volume: 12, Issue:7
| Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors. |
| AID1442527 | AUC (0 to 8 hrs) in Han-Wistar rat at 10 mg/kg, po measured after 15 to 480 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |