| Assay ID | Title | Year | Journal | Article |
|---|
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1189468 | Drug coverage index, ratio fCmax in in Wistar Han rat at 20 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189452 | Inhibition of LRRK2 G2910S mutant S1292 phosphorylation in BAC-transgenic mouse at 3 to 100 mg/kg, sc measured after 90 mins post dose | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189433 | Volume of distribution at steady state in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1604682 | Induction of neurogenesis in C57/BL6 mouse neural stem cells derived neurospheres isolated from adult ventricular-subventricular zone assessed as increase in neurosphere size at 1 to 5 uM measured after 4 days in presence of FGF or EGF by bright field mic | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Benzothiazole-Based LRRK2 Inhibitors as Wnt Enhancers and Promoters of Oligodendrocytic Fate. |
| AID1189434 | Oral bioavailability in rat at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189474 | Drug coverage index, ratio fAUC in in Wistar Han rat at 20 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189470 | fAUC in Wistar Han rat at 6 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189466 | fCmax in Wistar Han rat at 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189442 | Tmax in non-human primate at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189453 | Potency index, ratio of IC50 for LRRK2 G2910S mutant S395 phosphorylation in BAC-transgenic mouse at 3 to 100 mg/kg, sc to IC50 for wild type LRRK2 S395 phosphorylation in BAC-transgenic C57BL/6J mouse brain at 3 to 100 mg/kg, sc | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189475 | Drug coverage index, ratio fAUC in in Wistar Han rat at 60 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189473 | Drug coverage index, ratio fAUC in in Wistar Han rat at 6 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189431 | AUC in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189429 | Cmax in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189440 | Oral bioavailability in dog at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189471 | fAUC in Wistar Han rat at 20 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189427 | Inhibition of human recombinant MST4 using Ser/Thr peptide 7 substrate after 60 mins by Z-Lyte assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189465 | fCmax in Wistar Han rat at 20 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189469 | Drug coverage index, ratio fCmax in in Wistar Han rat at 60 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189455 | Toxicity in Wistar Han rat at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189436 | Tmax in dog at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189456 | Drug coverage index, ratio of average concentration ( 0 to 24 hrs) in in Wistar Han rat at 6 to 60 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189437 | AUC in dog at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189430 | Tmax in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189450 | Effect on total LRRK2 protein level in BAC-transgenic C57BL/6J mouse brain at 3 to 100 mg/kg, sc measured after 90 mins post dose | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189472 | fAUC in Wistar Han rat at 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189449 | Effect on total LRRK2 protein level in BAC-transgenic C57BL/6J mouse kidney at 3 to 100 mg/kg, sc measured after 90 mins post dose | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189424 | Clearance in rat liver microsomes | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1820722 | Displacement of K5 tracer from full length C-terminal NanoLuc fused human STK3 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia. |
| AID1189426 | Inhibition of human recombinant MST2 using Ser/Thr peptide 7 substrate after 45 mins by Z-Lyte assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189478 | Cytotoxicity against human THLE cells by in-vitro ATP depletion assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189458 | Toxicity in Wistar Han rat assessed as changes in electrolytes levels at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189460 | Toxicity in Wistar Han rat assessed as changes in body weight at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1604683 | Induction of neurogenesis in C57/BL6 mouse neural stem cells derived neurospheres isolated from adult ventricular-subventricular zone assessed as increase in total area of neurosphere at 1 to 5 uM measured after 4 days in presence of FGF or EGF by bright | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Benzothiazole-Based LRRK2 Inhibitors as Wnt Enhancers and Promoters of Oligodendrocytic Fate. |
| AID1189438 | Half life in dog at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189439 | Volume of distribution at steady state in dog at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189480 | Inhibition of JAK1 (JH2 domain-pseudokinase) (unknown origin) at 1 uM | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189447 | Inhibition of wild type LRRK2 S395 phosphorylation in BAC-transgenic C57BL/6J mouse brain at 3 to 100 mg/kg, sc measured after 90 mins post dose | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189459 | Toxicity in Wistar Han rat assessed as changes in food consumption at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1820724 | Displacement of K5 tracer from full length C-terminal NanoLuc fused human STK4 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia. |
| AID1604684 | Induction of neurogenesis in C57/BL6 mouse neuronal progenitor cells derived neurospheres isolated from adult ventricular-subventricular zone assessed as increase in neurosphere size at 1 to 5 uM measured after 4 days in presence of FGF or EGF by bright f | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Benzothiazole-Based LRRK2 Inhibitors as Wnt Enhancers and Promoters of Oligodendrocytic Fate. |
| AID1189479 | Inhibition of JAK1 (JH1 domain-catalytic) (unknown origin) at 1 uM | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189461 | Toxicity in Wistar Han rat assessed as changes in clinical chemistry parameters at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189444 | Half life in non-human primate at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189422 | Inhibition of full length LRRK2 (unknown origin) expressed in HEK293 cells assessed as reduction in S935 phosphorylation incubated for 90 mins by ELISA method | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189451 | Inhibition of LRRK2 G2910S mutant S395 phosphorylation in BAC-transgenic mouse at 3 to 100 mg/kg, sc measured after 90 mins post dose | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189481 | Inhibition of JAK2 (JH1 domain-catalytic) (unknown origin) at 1 uM | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189462 | Toxicity in Wistar Han rat assessed as changes in urinary biomarkers at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189446 | Oral bioavailability in non-human primate at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189441 | Cmax in non-human primate at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189464 | fCmax in Wistar Han rat at 6 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189476 | Inhibition of P-gp (unknown origin) assessed as efflux ratio | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189454 | Inhibition of LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189443 | AUC in non-human primate at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1820725 | Displacement of K5 tracer from full length C-terminal NanoLuc fused human LRRK2 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia. |
| AID1189445 | Volume of distribution at steady state in non-human primate at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189420 | Inhibition of GST-tagged truncated human recombinant LRRK2 using fluorescein-labeled LRRKtide peptide substrate incubated for 2 hrs | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189448 | Inhibition of wild type LRRK2 S395 phosphorylation in BAC-transgenic C57BL/6J mouse kidney at 3 to 100 mg/kg, sc measured after 90 mins post dose | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189435 | Cmax in dog at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189482 | Inhibition of JAK3 (JH1 domain-catalytic) (unknown origin) at 1 uM | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189457 | Toxicity in Wistar Han rat assessed as changes in RBC parameters at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189463 | Toxicity in Wistar Han rat assessed as changes in lung parameters at 6 to 60 mg/kg, po bid for 14 days by H and E staining method | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189477 | Apparent permeability from apical to basolateral side by cell based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189421 | Inhibition of GST-tagged truncated human recombinant LRRK2 G2019S mutant using fluorescein-labeled LRRKtide peptide substrate incubated for 90 mins | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189423 | Clearance in human liver microsomes | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189432 | Half life in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189467 | Drug coverage index, ratio fCmax in in Wistar Han rat at 6 mg/kg, po bid for 14 days to IC50 for LRRK2 S395 phosphorylation in Wistar Han rat brain at 6 to 60 mg/kg, po bid for 14 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| AID1189425 | Inhibition of LRRK2 in human PBMCs by ActivX KiNativ method | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| 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. |
| 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. |
| 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. |
| AID1345739 | Human leucine rich repeat kinase 2 (Leucine-rich repeat kinase (LRRK) family) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |