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. |
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. |
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. |
AID1153105 | Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153119 | Selectivity ratio of Ki for ROS1 (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153141 | AUC in rat CSF at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351349 | Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1351340 | Inhibition of ALK in human NCI-H3122 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1419634 | Inhibition of ALK (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1419630 | Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153136 | Tmax in rat at 10 mg/kg, po qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351350 | Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1153122 | Selectivity ratio of IC50 for FER (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419638 | Intrinsic absorptive permeability from basolateral side to apical side of dog RRCK cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1419629 | Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1419633 | Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153150 | Inhibition of LTK (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1680099 | Inhibition of EML4/ALK L1196M mutant (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1419640 | Efflux ratio in dog RRCK cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153093 | Inhibition of wild type human recombinant ALK kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobility sh | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351337 | Inhibition of ALK in human SU-DHL1 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1419624 | Inhibition of ROS1 G2032R mutant (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1680096 | Potency index, ratio of IC50 for crizotinib to lorlatinib IC50 for CD74-ROS1 (unknown origin) expressed in mouse BaF3 cells | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1680097 | Potency index, ratio of IC50 for crizotinib to lorlatinib IC50 for SLC34A2-ROS1 (unknown origin) expressed in human HCC78 cells | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1153094 | Inhibition of human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobilit | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153108 | Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153142 | fAUC in rat CSF at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1494500 | Inhibition of ALK L1196M mutant (unknown origin) | 2018 | Journal of medicinal chemistry, 08-09, Volume: 61, Issue:15
| Lipophilic Efficiency as an Important Metric in Drug Design. |
AID1153125 | Selectivity ratio of IC50 for TNK2 (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153138 | Average plasma concentration in rat at 10 mg/kg, po qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153100 | Efflux ratio of permeability from basolateral to apical side to apical to basolateral side of RRCK cells expressing BCRP at pH 7.4 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351344 | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1153102 | Selectivity ratio of Ki for TRKB (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153133 | Half life in rat at 1 mg/kg, iv qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153101 | Inhibition of TRKB (unknown origin) by off-chip mobility shift assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351343 | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1419626 | Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153134 | Cmax in rat at 10 mg/kg, po qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351345 | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1351339 | Inhibition of ALK in human NCI-H3122 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1351334 | Inhibition of ALK phosphorylation at Y1278 residue in human SU-DHL1 cells at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1351346 | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1419644 | Ratio of AUC in CSF to free plasma in rat | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153137 | AUC (0 to 24 hrs) in rat at 10 mg/kg, po qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351335 | Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1153120 | Selectivity ratio of Ki for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419639 | Intrinsic absorptive permeability from apical side to basolateral side of dog RRCK cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1680098 | Potency index, ratio of Ki for crizotinib to lorlatinib Ki for inhibition of ROS1 (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1419625 | Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153104 | Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153110 | Inhibition of ROS1 (unknown origin) by off-chip mobility shift assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153126 | Selectivity ratio of IC50 for PTK2 (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419636 | Octanol-water distribution coefficient, log D of the compound at pH 7.4 by RP-HPLC analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153112 | Inhibition of FES (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153145 | AUC in rat plasma at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153116 | Inhibition of NRTK1 (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153139 | Oral bioavailability in rat at 10 mg/kg qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419622 | Inhibition of wild type ROS1 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153132 | Volume of distribution at steady state in rat at 1 mg/kg, iv qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153117 | Inhibition of NRTK3 (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153127 | Selectivity ratio of IC50 for NTRK1 (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153131 | Plasma clearance in rat at 1 mg/kg, iv qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419637 | Intrinsic clearance in human liver microsomes | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153107 | Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153147 | Fraction unbound in rat brain at 2.4 uM | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153115 | Inhibition of PTK2 (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153096 | Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351348 | Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1680100 | Inhibition of ALK L1196M mutant (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1351342 | Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1680102 | Inhibition of ROS1 (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1351347 | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1494499 | Lipophilicity, log D of the compound | 2018 | Journal of medicinal chemistry, 08-09, Volume: 61, Issue:15
| Lipophilic Efficiency as an Important Metric in Drug Design. |
AID1419642 | Selectivity index, ratio of Ki for inhibition of TrkB (unknown origin) to KI for inhibition of ALK (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153121 | Selectivity ratio of IC50 for LTK (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153103 | Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419623 | Inhibition of ROS1 L2026M mutant (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153130 | AUC (infinity) in rat at 1 mg/kg, iv qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153135 | fCmax in rat at 10 mg/kg, po qd | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419643 | Oral bioavailability in rat | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1680095 | Potency index, ratio of Ki for crizotinib to lorlatinib Ki for inhibition of ALK L1196M (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1419635 | Inhibition of L1196M mutant (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1351311 | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1153143 | AUC in rat brain at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1351341 | Inhibition of ALK in human NCI-H3122 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1419632 | Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1680103 | Inhibition of SLC34A2-ROS1 (unknown origin) expressed in human HCC78 cells assessed as reduction in cell viability | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1153124 | Selectivity ratio of IC50 for PTK2B (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419628 | Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153106 | Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1680101 | Inhibition of CD74-ROS1 (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell viability | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
AID1153129 | Selectivity ratio of IC50 for FRK (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153144 | fAUC in rat brain at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153113 | Inhibition of PTK2B (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419645 | Ratio of fAUC in brain to plasma in rat | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1673958 | Inhibition of ROS1 L2026M mutant (unknown origin) in presence of ATP by microfluidic mobility shift assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1351338 | Inhibition of ALK phosphorylation at Y1278 residue in human NCI-H3122 cells at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID1153097 | Octanol-water distribution coefficient, Log D of the compound at pH 7.4 by HPLC-based shake-flask method | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153111 | Inhibition of FER (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153109 | Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153123 | Selectivity ratio of IC50 for FES (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419627 | Inhibition of wild type EML4/ALK C1156Y mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1419641 | Inhibition of TrkB (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1153099 | Efflux ratio of permeability from basolateral to apical side to apical to basolateral side of MDCK cells expressing MDR1 at pH 7.4 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153114 | Inhibition of TNK2 (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153140 | Fraction unbound in rat plasma at 2.4 uM | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153118 | Inhibition of FRK (unknown origin) by TR-FRET-based Z'-LYTE assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153095 | Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153128 | Selectivity ratio of IC50 for NTRK3 (unknown origin) to Ki for human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153146 | fAUC in rat plasma at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1153098 | Apparent total intrinsic clearance in human liver microsomes | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1419631 | Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
AID1351336 | Inhibition of ALK in human SU-DHL1 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 80 nM after 1 hr by Western blot analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
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. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 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. |
AID1345627 | Human FES proto-oncogene, tyrosine kinase (Fer family) | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID1345550 | Human ALK receptor tyrosine kinase (Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family) | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |