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Inhibition of ERK phosphorylation in human MIA PaCa-2 cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell growth
Antiproliferative activity against human NCI-H358
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 5 Tested
Inhibition of SOS1/KRAS G12C mutant (unknown origin) protein-protein interaction
Assay data:3 Active, 2 Activity ≤ 1 µM, 5 Tested
Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
Assay data:7 Active, 2 Activity ≤ 1 µM, 7 Tested
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
Assay data:5 Active, 3 Activity ≤ 1 µM, 7 Tested
Inhibition of KRAS G12C mutant (unknown origin) assessed as inhibition of SOS1-catalyzed nucleotide exchange measured by HTRF assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
HTRF Assay from US Patent US11345701: "KRAS mutant protein inhibitors"
Assay data:9 Active, 9 Activity ≤ 1 µM, 9 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Cytotoxicity against human NCI-H1373 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H2122 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H358 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by SRB assay
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay
Assay data:6 Active, 3 Activity ≤ 1 µM, 9 Tested
Antiproliferative activity against human NCI-H358 cells
Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in p-ERK levels
Unbound plasma concentration in athymic nude mouse xenografted with human MIAPaCa2 cells at 10 mg/kg, po qd after 8 hrs post-last dose
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Antiproliferative activity against human MIAPaCa2 cells harboring KRAS G12C point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay
Assay data:21 Active, 1 Activity ≤ 1 nM, 21 Activity ≤ 1 µM, 21 Tested
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