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In vitro Assay from US Patent US20240018122: "PYRIDAZINYL AMINO DERIVATIVES AS ALK5 INHIBITORS"
Assay data:187 Active, 157 Activity ≤ 1 nM, 186 Activity ≤ 1 µM, 188 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
No assay from US Patent US11759530: "TKI permeability enhancers"
Assay data:9 Active, 9 Activity ≤ 1 µM, 11 Tested
LanthaScreen Eu Kinase Binding Assay from US Patent US11746103: "ALK-5 inhibitors and uses thereof"
Assay data:8 Active, 56 Activity ≤ 1 µM, 56 Tested
In Vitro Kinase Assay - Inhibition of ALK1/2/3/4/5/6 Kinases from US Patent US11702401: "Compounds and methods of use"
Assay data:33 Active, 32 Activity ≤ 1 µM, 36 Tested
TGFβR1 Kinase Inhibition Assay from US Patent US11691981: "Heterocyclic compounds, preparation methods therefor, and methods of uses thereof"
Assay data:79 Active, 76 Activity ≤ 1 µM, 80 Tested
Luciferase Reporter Gene Assay for ALK2 and TGFbeta Activity from US Patent US11654147: "ALK2 inhibitors and methods for inhibiting BMP signaling"
Assay data:149 Active, 1 Activity ≤ 1 nM, 165 Activity ≤ 1 µM, 170 Tested
Enzyme Activity Inhibition from US Patent US11584745: "Aromatic heterocyclic compound, intermediate thereof, preparation method therefor, and pharmaceutical composition and use thereof"
Assay data:14 Active, 13 Activity ≤ 1 µM, 15 Tested
Inhibition of human TGF-beta-R1 using TMB substrate incubated for 2.5 hrs by microplate reader analysis
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Selectivity interaction (KinomeScan (DiscoverX)) EUB0000252b TGFBR1
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b TGFBR1
Affinity Biochemical interaction (Lathascreen (Takeda)) EUB0000312b TGFBR1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000710a TGFBR1
Affinity On-target Cellular interaction (Reporter gene assay) EUB0000312b TGFBR1
Affinity Phenotypic Cellular interaction (Western blot (inhibition of SMAD2/3 phosphorylation)) EUB0000710a TGFBR1
Affinity Phenotypic Cellular interaction (Western blot (inhibition of SMAD2/3 phosphorylation)) EUB0000312b TGFBR1
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of TGFBR1 (unknown origin) at 50 nM by Z'LYTE screening method relative to control
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of ALK5 (unknown origin)
Assay data:23 Active, 24 Activity ≤ 1 µM, 24 Tested
Inhibition of TGF-beta receptor 1 in human RD cells transfected with Smad reporter plasmid by reporter gene based One-Glo luciferase assay
Assay data:3 Active, 12 Activity ≤ 1 µM, 12 Tested
Displacement of Alexa Fluor labeled tracer 178 from ALK5 (unknown origin) using anti-GST antibody incubated for 60 mins by TR-FRET based LanthaScreen Eu-Kinase binding assay
Assay data:2 Active, 12 Activity ≤ 1 µM, 12 Tested
Inhibition of recombinant human GST-tagged full length ALK5 expressed in baculovirus assessed as loss of peptide phosphorylation activity using peptide substrate in presence of ATP and measured after 1 hrs by HTRF assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
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