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In Vitro Assay from US Patent US20230312576: "4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-3,6-DIHYDROPYRIDINE-1-(2H)-CARBOXAMIDE DERIVATIVES AS LIMK AND/OR ROCK KINASES INHIBITORS FOR USE IN THE TREATMENT OF CANCER"
Assay data:118 Active, 114 Activity ≤ 1 µM, 118 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (DSF assay) EUB0000285b LIMK1
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (ScanMAX (DiscoverX, competition-binding assay)) EUB0000232b LIMK1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Selectivity interaction (Kinobead pulldown assay ) EUB0000232b LIMK1
Selectivity interaction (DSF assay) EUB0000232b LIMK1
Affinity Biochemical interaction (RapidFire MS assay) EUB0000285b LIMK1
Affinity Biochemical interaction (RapidFire MS assay) EUB0000232b LIMK1
Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000285b LIMK1
Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000232b LIMK1
Inhibition of LIMK1 (unknown origin)
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of LIMK1 (unknown origin) at 1.0 uM relative to control
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of LIMK1 (unknown origin) at 1 uM relative to control
Inhibition of human LIMK1 at 1 uM relative to control
Inhibition of LIMK1/LIMK2 in human SH-SY5Y cells assessed as effect on phospho cofilin serine 3 phosphorylation incubated for 2 hr by AlphaLISA SureFire assay
Assay data:11 Active, 11 Activity ≤ 1 µM, 17 Tested
Inhibition of recombinant LIMK1(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay
Assay data:12 Active, 11 Activity ≤ 1 µM, 17 Tested
Inhibition of PAK mediated recombinant LIMK1 phosphorylation (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay
Assay data:19 Active, 13 Activity ≤ 1 µM, 21 Tested
Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay
Assay data:19 Active, 18 Activity ≤ 1 µM, 21 Tested
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of GST tagged recombinant LIMK1 (unknown origin) using cofilin as substrate by by SDS-PAGE analysis
Inhibition of his6 tagged LIMK1 (unknown origin) expressed in baculovirus-infected Sf9 cells measured after 1 hr in presence of ATP by fluorescence based analysis
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