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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
RAF1 Invitrogen Lab (UK) kinase screen (BI)
Assay data:1 Tested
Inhibition of c-RAF (unknown origin) at 10 uM by biochemical hotspot kinase assay relative to control
SummaryPubMed CitationRelated BioAssays by Target
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
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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 RAF1 (unknown origin) at 10 uM using magnesium acetate as substrate incubated for 40 mins in presence of [gamma33P]ATP by scintillation counting based hotspot kinase assay relative to control
Assay data:4 Tested
Inhibition of RAF1 (unknown origin) using magnesium acetate as substrate incubated for 40 mins in presence of [gamma33P]ATP by scintillation counting based hotspot kinase assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
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