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Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of Trk-A F595R mutant (unknown origin) incubated for 30 mins by caliper mobility shift assay
Assay data:13 Active, 1 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 18 Tested
Inhibition of wild type TRAK (unknown origin) incubated for 30 mins by caliper mobility shift assay
Assay data:15 Active, 3 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of wild type TRKA (unknown origin)
Assay data:17 Active, 2 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 18 Tested
Inhibition of TRKA F589L mutant (unknown origin) using TK-sub biotin peptide substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins by FRET assay
Assay data:13 Active, 4 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 13 Tested
Inhibition of wildtype human TRKA using poly (Glu,Tyr) 4:1 as substrate in presence of [gamma-33P]ATP by hotspot kinase assay
Assay data:6 Active, 2 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
Inhibition of TRKA F589L mutant (unknown origin) preincubated for 30 mins followed by biotinylated TK-peptide substrate addition and measured after 40 mins by FRET-based Z-lyte kinase assay
Assay data:7 Active, 4 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate in presence of ATP by radiometric HotSpot kinase assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human TRKC using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay
Inhibition of human TRKB using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay
Inhibition of ROS1 (unknown origin) incubated for 120 mins in presence of 33P-ATP
Assay data:5 Active, 3 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Inhibition of TrKC (unknown origin) incubated for 120 mins in presence of 33P-ATP
Assay data:5 Active, 5 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Inhibition of human TRKA using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay
Kinase Binding Assays from US Patent US10618912: "Diaryl macrocycles as modulators of protein kinases"
Assay data:18 Active, 13 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Kinase Binding Assays from US Patent US10246466: "Diaryl macrocycles as modulators of protein kinases"
Inhibition of LMNA-TRKA G595R (unknown origin) expressed in mouse Ba/F3 cells assessed as antiproliferative activity incubated for 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Inhibition of TRKC G625R mutant (unknown origin)
Inhibition of TRKA G595R mutant (unknown origin)
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