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KRAS G12C-GDP Exchange Assay from US Patent US20240109893: "PREPARATION AND APPLICATION METHOD OF HETEROCYCLIC COMPOUNDS AS KRAS INHIBITOR"
Assay data:22 Active, 8 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 22 Tested
SummaryRelated BioAssays by Target
SOS1 GDP TR-FRET Assay from US Patent US20240092803: "BRIDGED COMPOUNDS AS KRAS G12D INHIBITOR AND DEGRADER AND THE USE THEREOF"
Assay data:14 Active, 12 Activity ≤ 1 µM, 15 Tested
Biochemical Assay 3 from US Patent US20240083857: "2-Methyl-Quinazolines"
Assay data:314 Active, 144 Activity ≤ 1 µM, 367 Tested
Biochemical Assay 2 from US Patent US20240083857: "2-Methyl-Quinazolines"
Assay data:367 Active, 181 Activity ≤ 1 µM, 395 Tested
Biochemical Assay 1 from US Patent US20240083857: "2-Methyl-Quinazolines"
Assay data:372 Active, 198 Activity ≤ 1 µM, 401 Tested
Coupled Nucleotide Exchange Assay from US Patent US20240059703: "HETEROCYCLIC SPIRO COMPOUNDS AND METHODS OF USE"
Assay data:506 Active, 473 Activity ≤ 1 µM, 513 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
KRAS::SOS1 AlphaScreen Binding Assay from US Patent US20240051956: "SOS1 INHIBITORS AND USES THEREOF"
Assay data:85 Active, 87 Activity ≤ 1 µM, 87 Tested
SOS-Catalyzed Nucleotide Exchange Assay from US Patent US20240043448: "Small Molecule Inhibitors of KRAS G12C Mutant"
Assay data:93 Active, 7 Activity ≤ 1 nM, 83 Activity ≤ 1 µM, 93 Tested
In vivo protac activity at VHL/AR in human VCaP cells xenografted SCID mouse assessed as reduction in PSA protein level in tumor at 50 mg/kg, ip administered as single dose measured after 3 to 48 hrs Western blot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with proteasome inhibitor, MG132 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with NEDD8 activating E1 enzyme inhibitor, MLN4924 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with VHL ligand, (2S,4R)-4-hydroxy-1-((R)-3-methyl-2-(3-methylisoxazol-5-yl)butanoyl)-N-((S)-3-(methylamino)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)pyrrolidine-2-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with N-((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with proteasome inhibitor, MG132 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with NEDD8 activating E1 enzyme inhibitor, MLN4924 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with VHL ligand, (2S,4R)-4-hydroxy-1-((R)-3-methyl-2-(3-methylisoxazol-5-yl)butanoyl)-N-((S)-3-(methylamino)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)pyrrolidine-2-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with N-((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in human VCaP cells assessed as induction of protein degradation at 10 nM measured after 24 hrs by Western blot analysis relative to control
Protac activity at VHL/AR in human 22Rv1 cells assessed as induction of protein degradation measured after 24 hrs by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Protac activity at VHL/AR in human VCaP cells assessed as induction of protein degradation measured after 24 hrs by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
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