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HTS to identify compounds that affect the blood-brain barrier permeability in vitro
Assay data:419 Active, 1260 Tested
SummaryCompounds, Active
Selectivity interaction (ScanMAX (DiscoverX, competition-binding assay)) EUB0000232b LIMK1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (Kinobead pulldown assay ) EUB0000232b LIMK1
Affinity Biochemical interaction (RapidFire MS assay) EUB0000232b LIMK1
Affinity Biochemical interaction (RapidFire MS assay) EUB0000232b LIMK2
Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000232b LIMK1
Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000232b LIMK2
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant LIMK2(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay
Assay data:12 Active, 12 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 LIMK2 phosphorylation (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay
Assay data:17 Active, 13 Activity ≤ 1 µM, 21 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 LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay
Assay data:17 Active, 14 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
Binding affinity to human wild-type full length LIMK2 (M1 to P638 residues) expressed in bacterial expression system assessed as dissociation constant by Kinomescan method
Binding affinity to human wild-type full length LIMK1 (M1 to D647 residues) expressed in bacterial expression system assessed as dissociation constant by Kinomescan method
Binding affinity to LIMK2 in human HeLa cells assessed as apparent dissociation constant incubated for 45 mins by kinobead based pulldown assay
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Binding affinity to LIMK1 in human HeLa cells assessed as apparent dissociation constant incubated for 45 mins by kinobead based pulldown assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of LIMK2 in human HeLa cells lysate incubated for 45 mins by kinobead based pulldown assay
Inhibition of LIMK1 in human HeLa cells lysate incubated for 45 mins by kinobead based pulldown assay
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