BDBM657592 6,7-dimethoxy-2-methyl-N-[1-(4-{2-[(methylamino)methyl]phenyl}thiophen-2-yl)ethyl]quinazolin-4-amine::US20240083857, Example 271::US20240083857, Example 326::US20240083857, Example 327
SMILES CNCc1ccccc1-c1csc(c1)C(C)Nc1nc(C)nc2cc(OC)c(OC)cc12
InChI Key InChIKey=WEGLOYDTDILXDA-UHFFFAOYSA-N
Data 12 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 27 hits for monomerid = 657592
Affinity DataIC50: 12.9nMAssay Description:The expression and purification of N-terminal GST-tagged human K-RasG120 and N-terminal His-tagged human SOS1 is described below. Concentrations of p...More data for this Ligand-Target Pair
Affinity DataKd: 18nMAssay Description:Binding affinity to N-terminal His10-tagged wild-type recombinant human SOS1 catalytic domain (564 to 1049 residues) expressed in Escherichia coli as...More data for this Ligand-Target Pair
Affinity DataIC50: 27.7nMAssay Description:This assay quantifies human SOS1-mediated loading of human K-RasG12C-GDP with a fluorescent GTP-analog. Detection of successful loading is achieved b...More data for this Ligand-Target Pair
Affinity DataIC50: 29.1nMAssay Description:Preparation of GST-tagged hK-RasGl2C loaded with fluorescent nucleotide was performed as follows: incubation of 11.5 μM hK-RasGl2C with 5-fold e...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human KRAS G12C mutant (1 to 169 residues) expressed in Escherichia coli/N-terminal His10-tagged wild...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human KRAS G12C mutant (1 to 169 residues) expressed in Escherichia coli/N-terminal His10-tagged wild...More data for this Ligand-Target Pair
Affinity DataIC50: 60.5nMAssay Description:The expression and purification of N-terminal GST-tagged human K-RasG120 and N-terminal His-tagged human SOS1 is described below. Concentrations of p...More data for this Ligand-Target Pair
Affinity DataIC50: 61nMAssay Description:Inhibition of N-terminal His10-tagged wild-type recombinant human SOS1 catalytic domain (564 to 1049 residues) expressed in Escherichia coli assessed...More data for this Ligand-Target Pair
Affinity DataIC50: 72.6nMAssay Description:Preparation of GST-tagged hK-RasGl2C loaded with fluorescent nucleotide was performed as follows: incubation of 11.5 μM hK-RasGl2C with 5-fold e...More data for this Ligand-Target Pair
Affinity DataIC50: 75.9nMAssay Description:This assay quantifies human SOS1-mediated loading of human K-RasG12C-GDP with a fluorescent GTP-analog. Detection of successful loading is achieved b...More data for this Ligand-Target Pair
Affinity DataIC50: 91nMAssay Description:Inhibition of N-terminal His10-tagged wild-type recombinant human SOS1 catalytic domain (564 to 1049 residues) expressed in Escherichia coli assessed...More data for this Ligand-Target Pair
Affinity DataIC50: 94nMAssay Description:Inhibition of N-terminal His10-tagged wild-type recombinant human SOS1 catalytic domain (564 to 1049 residues) expressed in Escherichia coli assessed...More data for this Ligand-Target Pair
Affinity DataIC50: 190nMAssay Description:Inhibition of SOS1 in human MOLM-13 cells assessed as reduction in pERK level incubated for 60 mins by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 260nMAssay Description:Inhibition of SOS1 in human K562 cells assessed as reduction in pERK level incubated for 60 mins by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 360nMAssay Description:Inhibition of SOS1 in human Calu-1 cells assessed as reduction in pERK level incubated for 24 hrs by HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 410nMAssay Description:Inhibition of SOS1 in human Calu-1 cells assessed as reduction in RAS activation pretreated for 30 mins followed by EGF stimulation for 3 mins by G-L...More data for this Ligand-Target Pair
Affinity DataIC50: 1.32E+3nMAssay Description:Inhibition of SOS1 in human HeLa cells assessed as reduction in RAS activation pretreated for 30 mins followed by EGF stimulation for 3 mins by G-LIS...More data for this Ligand-Target Pair
Affinity DataIC50: 1.38E+3nMAssay Description:The expression and purification of N-terminal GST-tagged human K-RasG120 and N-terminal His-tagged human SOS1 is described below. Concentrations of p...More data for this Ligand-Target Pair
Affinity DataIC50: 1.94E+3nMAssay Description:Preparation of GST-tagged hK-RasGl2C loaded with fluorescent nucleotide was performed as follows: incubation of 11.5 μM hK-RasGl2C with 5-fold e...More data for this Ligand-Target Pair
Affinity DataIC50: 2.56E+3nMAssay Description:This assay quantifies human SOS1-mediated loading of human K-RasG12C-GDP with a fluorescent GTP-analog. Detection of successful loading is achieved b...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human KRAS G12C mutant (1 to 169 residues) expressed in Escherichia coli assessed as reduction in int...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of human DBS assessed as reduction in CDC42 activation preincubated for 1 min with CDC42 followed by DBS addition measured after 20 mins i...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of human EGFR using biotin-aminohexyl-AEEEEYFELVAKKK as substrate preincubated for 15 mins followed by substrate/ATP addition measured aft...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of N-terminal His10-tagged wild-type recombinant human SOS2 catalytic domain (564 to 1043 residues) expressed in Escherichia coli assessed...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair