BDBM412687 US10399979, Compound 18
SMILES COc1cc2c3cnc4[nH]ccc4c3n([C@@H]3CCCN(C3)C(=O)CC#N)c(=O)c2cc1OC
InChI Key
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 13 hits for monomerid = 412687
Affinity DataIC50: 1.02nMAssay Description:Reagents used in JAK inhibition assay: Base Reaction buffer; 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO...More data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 3.12nMAssay Description:Reagents used in JAK inhibition assay: Base Reaction buffer; 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO...More data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 2.55nMAssay Description:Reagents used in JAK inhibition assay: Base Reaction buffer; 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO...More data for this Ligand-Target Pair
Ligand Info
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Purdue Research Foundation
US Patent
Purdue Research Foundation
US Patent
Affinity DataIC50: 4.35nMAssay Description:Reagents used in JAK inhibition assay: Base Reaction buffer; 20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO...More data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 3.10nMAssay Description:Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding methodMore data for this Ligand-Target Pair
Ligand Info
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Purdue Research Foundation
US Patent
Purdue Research Foundation
US Patent
Affinity DataIC50: 4.40nMAssay Description:Inhibition of TYK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding methodMore data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 2.60nMAssay Description:Inhibition of JAK3 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding methodMore data for this Ligand-Target Pair
Ligand Info
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Purdue University
Curated by ChEMBL
Purdue University
Curated by ChEMBL
Affinity DataKd: >100nMAssay Description:Binding affinity to DNA-tagged recombinant human FLT3 D835V mutant (592 to 969 residues) expressed in mammalian expression system by KINOMEscan assayMore data for this Ligand-Target Pair
Target InfoPDBNCI pathwayReactome pathway
UniProtKB/SwissProt
B.MOADDrugBankantibodypediaGoogleScholar
UniProtKB/SwissProt
B.MOADDrugBankantibodypediaGoogleScholar
Ligand Info
TargetMitogen-activated protein kinase kinase kinase 19(Homo sapiens (Human))
Purdue University
Curated by ChEMBL
Purdue University
Curated by ChEMBL
Affinity DataKd: 1.20nMAssay Description:Binding affinity to DNA-tagged recombinant human YSK4 (1019 to 1328 residues) expressed in mammalian expression system by KINOMEscan assayMore data for this Ligand-Target Pair
Ligand Info
Affinity DataKd: 0.220nMAssay Description:Binding affinity to DNA-tagged recombinant human BIKE (34 to 329 residues) expressed in bacterial expression system by KINOMEscan assayMore data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 1.55E+3nMAssay Description:Inhibition of JAK3 in human SZ4 cells assessed as reduction in IL2-stimulated STAT5 phosphorylation preincubated for 1 hr followed by IL2 stimulation...More data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 1.20nMAssay Description:Inhibition of JAK1 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding methodMore data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 15nMAssay Description:Inhibition of JAK3 in human SZ4 cells assessed as reduction in IL2-stimulated STAT5 phosphorylation preincubated for 1 hr followed by IL2 stimulation...More data for this Ligand-Target Pair
Ligand Info