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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
SummaryRelated 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
Inhibition of KRAS G12C mutant in human MIA PaCa-2 cells assessed as reduction in whole blood pERK level incubated for 4 hrs by HTRF assay
Assay data:6 Activity ≤ 1 µM, 6 Tested
Inhibition of KRAS G12C mutant in human MIA PaCa-2 cells assessed as reduction in pERK level incubated for 4 hrs by HTRF assay
Inhibition of KRAS G12C mutant (unknown origin) assessed as inhibition of SOS1 mediated nucleotide exchange incubated for 2 hrs in presence of GppNHp by fluorescence based analysis
Protac activity at VHL/KRAS G12D in human ASPC1 cells assessed as induction of KRAS G12D protein degradation at 1 uM incubated for 24 hrs by luminescence based analysis relative to control
Assay data:6 Tested
Inhibition of KRAS G12D mutant in human ASPC1 cells assessed as reduction in ERK1/2 phosphorylation level incubated for 2 hrs by MSD assay
Assay data:12 Active, 12 Activity ≤ 1 µM, 12 Tested
Inhibition of N-terminal His-tagged GDP-bound KRAS G12D mutant (1 to 169 residues) (unknown origin) assessed as inhibition of SOS mediated nucleotide exchange preincubated for 2 hrs followed by addition of SOS protein and unlabeled GTP measured after 30 mins by Alphascreen assay
Assay data:12 Active, 4 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
Inhibition of His-tagged KRAS G12D mutant (unknown origin) using biotinylated KRPep-2d as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by LANCE TR-FRET assay
Assay data:12 Active, 7 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
Inhibition of GTP bound KRAS G12D mutant in human GP2d cells assessed as reduction in pERK level incubated for 3 hrs
Assay data:12 Activity ≤ 1 µM, 12 Tested
Inhibition of KRAS G12V mutant (unknown origin) preincubated for 4 hrs followed by SOS1 addition and measured after 3 hrs by fluorescence based analysis
Inhibition of KRAS G12D mutant (unknown origin) preincubated for 4 hrs followed by SOS1 addition and measured after 2 hrs by fluorescence based analysis
Inhibition of KRAS (unknown origin) to CRAF (unknown origin) protein protein interaction
Assay data:3 Active, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of human KRAS G12D mutant in human AGS cells assessed as reduction in phosphorylated ERK level incubated for 3 hrs
Assay data:2 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
Protac activity at VHL/KRAS G12C mutant in human NCI-H358 cells assessed as degradation of KRAS G12C mutant incubated for 24 hrs by immunoblot assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Protac activity at VHL/KRAS G12C mutant in human NCI-H23 cells assessed as degradation of KRAS G12C mutant incubated for 24 hrs by immunoblot assay
Protac activity at VHL/KRAS G12C mutant in human SW1573 cells assessed as degradation of KRAS G12C mutant incubated for 24 hrs by immunoblot assay
Protac activity at VHL/KRAS G12C mutant in human MIA PaCa-2 cells assessed as degradation of KRAS G12C mutant incubated for 24 hrs by immunoblot assay
Protac activity at VHL/KRAS G12C mutant in human NCI-H2030 cells assessed as degradation of KRAS G12C mutant incubated for 24 hrs by immunoblot assay
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