BDBM2579 (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one::CHEMBL388978::Staurosporin, 4::Staurosporine::Staurosporine, 8::US11958831, Example Staurosporine::US20240002365, Compound staurosporine::US9206188, Staurosporine::US9226923, Staurosporine
SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13
InChI Key InChIKey=HKSZLNNOFSGOKW-FYTWVXJKSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 2368 hits for monomerid = 2579
Affinity DataKi: 1nM ΔG°: -12.1kcal/molepH: 7.4 T: 22°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
Affinity DataKi: 2.20nM ΔG°: -11.8kcal/molepH: 8.0 T: 25°CAssay Description:Assays were performed for the Itk enzyme containing residues 357-620, and an Itk enzyme containing the catalytic kinase domain and the TH and SH2 dom...More data for this Ligand-Target Pair
Affinity DataKi: 2.60nMAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataKi: 2.90nM ΔG°: -11.5kcal/molepH: 7.4 T: 22°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
Affinity DataKi: 4nMAssay Description:Inhibition of CDK2/Cyclin A (174 to 432 amino acid residues) (unknown origin) by differential scanning fluorimetry assayMore data for this Ligand-Target Pair
Affinity DataKi: 7nMAssay Description:Inhibition of CDK9/Cyclin T (1 to 330 amino acid residues) (unknown origin) by differential scanning fluorimetry assayMore data for this Ligand-Target Pair
Affinity DataKi: 7.80nM ΔG°: -11.5kcal/molepH: 7.4 T: 37°CAssay Description:In vitro Chk1 enzymatic assay using purified enzyme, was incubated with substrate, and test compounds in the presence of 10 uM ATP/ [gamma-32P] ATP. ...More data for this Ligand-Target Pair
Affinity DataKi: <10nM ΔG°: <-10.9kcal/molepH: 8.0 T: 25°CAssay Description:Assays were performed for the Itk enzyme containing residues 357-620, and an Itk enzyme containing the catalytic kinase domain and the TH and SH2 dom...More data for this Ligand-Target Pair
Affinity DataKi: 19nM ΔG°: -10.7kcal/moleT: 30°CAssay Description:Protein kinase C (PKC) enzyme inhibition assay using purified rat brain protein kinase C from Calbiochem #539494.More data for this Ligand-Target Pair
Affinity DataKi: 35nMpH: 7.5Assay Description:Cyclic AMP-dependent protein kinase (PKA) enzyme inhibition assay using purified recombinant C subunit of PKA (catalytic (C) subunit (cPKA)) with hol...More data for this Ligand-Target Pair
Affinity DataKi: 41nM ΔG°: -10.2kcal/molepH: 7.5 T: 30°CAssay Description:CDK4 and cyclin D1 were expressed in a baculovirus expression system and subsequently purified. The catalytic activity of the CDK4 protein was assaye...More data for this Ligand-Target Pair
Affinity DataKi: 150nMAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataKi: 790nM ΔG°: -8.24kcal/molepH: 7.5 T: 22°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataKi: 1.20E+3nMAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMpH: 7.2 T: 30°CAssay Description:The activity of MLCK is measured by its ability to transfer 32P from [gamma-32P]ATP to myosin light-chain.More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:The activity of PKC, activated by phosphatidylserine and Ca2+, is measured by its ability to transfer phosphate from [gamma-32P]ATP to lysine-rich hi...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:The activity of PKA, activated by cAMP, is measured by its ability to transfer phosphate from [gamma-32P]ATP to histone.More data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:The activity of cGPK, activated by cGMP, is measured by its ability to transfer phosphate from [gamma-32P]ATP to histone.More data for this Ligand-Target Pair
Affinity DataIC50: 400nMAssay Description:The activity of TPK is measured by its ability to transfer 32P from [gamma-32P]ATP to Poly(Glu,Tyr; 4:l).More data for this Ligand-Target Pair
Affinity DataIC50: 9nMpH: 7.5 T: 30°CAssay Description:The activity of PKC, activated by phosphatidylerine and Ca2+, is measured by its ability to transfer phosphate from [gamma-32P]ATP to lysine-rich his...More data for this Ligand-Target Pair
Affinity DataIC50: 9nMpH: 7.5 T: 30°CAssay Description:The activity of PKC, activated by phosphatidylerine and Ca2+, is measured by its ability to transfer phosphate from [gamma-32P]ATP to lysine-rich his...More data for this Ligand-Target Pair
Affinity DataIC50: 121nMpH: 8.5 T: 37°CAssay Description:The activity of PKA, activated by cAMP, is measured by its ability to transfer phosphate from [gamma-32P]ATP to histone.More data for this Ligand-Target Pair
Affinity DataIC50: 59nMpH: 7.0 T: 22°CAssay Description:In vitro CDK assay using purified enzyme, was incubated at room temperature with substrate, and test compounds in the presence of ATP/[gamma-33P]ATP....More data for this Ligand-Target Pair
Affinity DataIC50: <45nMpH: 6.8 T: 25°CAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 47nMpH: 6.8 T: 25°CAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [V123M](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMpH: 6.8 T: 25°CAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [E127D](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I,Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [V123M,Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I,V123M,Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 51nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I,V123M,E127D,Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: <45nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:The kinase activity was determined by incubation of enzyme and its substrate, and test compound, in the presence ATP/[gamma-33P] ATP. After incubatio...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMpH: 7.6 T: 30°CAssay Description:A coupled-enzyme assay was used to quantify the ADP generated in the kinase reaction with S6 peptide (RRRLSSLRA) as the phosphoacceptorsubstrate.More data for this Ligand-Target Pair
Affinity DataIC50: 57nMpH: 7.5 T: 22°CAssay Description:The full-length cFMS cytoplasmic domain (FMS.538-972.6His) or chimera was incubated with compound in reaction buffer. Control reactions were run in e...More data for this Ligand-Target Pair
TargetMacrophage colony-stimulating factor 1 receptor [538-678,753-922](Human)
Johnson & Johnson Pharmaceutical
Johnson & Johnson Pharmaceutical
Affinity DataIC50: 49nMpH: 7.5 T: 22°CAssay Description:The full-length cFMS cytoplasmic domain (FMS.538-972.6His) or chimera was incubated with compound in reaction buffer. Control reactions were run in e...More data for this Ligand-Target Pair
TargetMacrophage colony-stimulating factor 1 receptor [538-678,753-922](Human)
Johnson & Johnson Pharmaceutical
Johnson & Johnson Pharmaceutical
Affinity DataIC50: 57nMpH: 7.5 T: 22°CAssay Description:The full-length cFMS cytoplasmic domain (FMS.538-972.6His) or chimera was incubated with compound in reaction buffer. Control reactions were run in e...More data for this Ligand-Target Pair
Affinity DataIC50: 6.5nMpH: 7.5 T: 30°CAssay Description:In vitro PDK1 assay using purified enzyme, was incubated with substrate PDKtide, and test compounds in the presence of ATP/ [gamma-32P] ATP. 32P inco...More data for this Ligand-Target Pair
TargetRAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D](Human)
Abbott Laboratories
Abbott Laboratories
Affinity DataIC50: 1.5nMpH: 7.5 T: 22°CAssay Description:The kinase assay uses His-Akt1 and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidin-coated FLASH plat...More data for this Ligand-Target Pair
Affinity DataIC50: 6.5nMpH: 7.5 T: 22°CAssay Description:The kinase assay uses His-Akt1 and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidin-coated FLASH plat...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMpH: 7.5 T: 22°CAssay Description:The kinase assay uses His-Akt1 and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidin-coated FLASH plat...More data for this Ligand-Target Pair
Affinity DataIC50: 3.60nMpH: 7.4 T: 22°CAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
Affinity DataIC50: 6.60nMpH: 7.4 T: 22°CAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
Affinity DataIC50: 570nMpH: 7.4 T: 22°CAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
Affinity DataIC50: 9.00E+3nM Kd: 290nMpH: 7.2 T: 20°CAssay Description:Binding was detected as a change in the intrinsic tryptophan fluorescence of the PI3K upon the addition of inhibitor. The inhibitor was incubated wit...More data for this Ligand-Target Pair
Affinity DataIC50: 240nMpH: 7.5 T: 24°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
Affinity DataIC50: 80nMpH: 7.5 T: 30°CAssay Description:NSC 109555 was diluted in water. All other drugs were dissolved in DMSO, in which case the final DMSO concentration in reactions was 10%, and the con...More data for this Ligand-Target Pair
Affinity DataIC50: 4.53E+3nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
Affinity DataIC50: 1.06E+4nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
Activity Spreadsheet -- ITC Data from BindingDB
Found 1 hit for monomerid = 2579
ITC DataΔG°: -11.5kcal/mole −TΔS°: -3.33kcal/mole ΔH°: -8.09kcal/mole logk: 7.05E+8
pH: 7.5 T: 10.00°C
pH: 7.5 T: 10.00°C