BDBM2583 3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione::3,4-bis(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione::BIM-4::Bisindolyl deriv. 3::Bisindolylmaleimide deriv. 5::CHEMBL266487::bis-indolylmaleimide deriv. 8a
SMILES: O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12
InChI Key: InChIKey=DQYBRTASHMYDJG-UHFFFAOYSA-N
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Protein Kinase C (Rattus norvegicus (rat)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 550 | n/a | n/a | n/a | n/a | 7.5 | 30 |
Roche Products Limited | Assay 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... | J Med Chem 35: 177-84 (1992) Article DOI: 10.1021/jm00079a024 BindingDB Entry DOI: 10.7270/Q2K64G8V | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Cyclin B/Cyclin-Dependent Kinase 1 (CDK1)/G2/mitotic-specific cyclin B2/G2/mitotic-specific cyclin B3 (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB UniProtKB/SwissProt antibodypedia antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 1.80E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Kyushu University Curated by ChEMBL | Assay Description Inhibitory concentration was determined by measuring phoshporylation of H1 histone using active human Cell division cycle 2-cyclin B complex | Bioorg Med Chem Lett 8: 1019-22 (1999) BindingDB Entry DOI: 10.7270/Q27W6BBN | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
cAMP-Dependent Protein Kinase (PKA) (Bos taurus (bovine)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 100 | n/a | n/a | n/a | n/a | 7.4 | 30 |
Laboratoires Glaxo | Assay Description IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe... | J Biol Chem 266: 15771-81 (1991) BindingDB Entry DOI: 10.7270/Q2FF3QJ4 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
cAMP-Dependent Protein Kinase (PKA) (Rattus norvegicus (rat)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB Reactome pathway UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 2.00E+3 | n/a | n/a | n/a | n/a | 7.0 | 30 |
Laboratoires Glaxo | Assay Description IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe... | J Biol Chem 266: 15771-81 (1991) BindingDB Entry DOI: 10.7270/Q2FF3QJ4 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Phosphorylase Kinase (Oryctolagus cuniculus (rabbit)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 3.20E+3 | n/a | n/a | n/a | n/a | 7.0 | 30 |
Laboratoires Glaxo | Assay Description IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe... | J Biol Chem 266: 15771-81 (1991) BindingDB Entry DOI: 10.7270/Q2FF3QJ4 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Cyclin-Dependent Kinase 4 (CDK4) (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 5.81E+3 | n/a | n/a | n/a | n/a | 7.0 | 22 |
DCR&T, Lilly Spain S.A. | Assay 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.... | Bioorg Med Chem Lett 13: 3841-6 (2003) Article DOI: 10.1016/S0960-894X(03)00792-3 BindingDB Entry DOI: 10.7270/Q2FN14C5 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
CDK2/CycE (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB UniProtKB/SwissProt UniProtKB/TrEMBL antibodypedia antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 1.17E+4 | n/a | n/a | n/a | n/a | n/a | 25 |
DCR&T, Lilly Spain S.A. | Assay 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.... | Bioorg Med Chem Lett 13: 3841-6 (2003) Article DOI: 10.1016/S0960-894X(03)00792-3 BindingDB Entry DOI: 10.7270/Q2FN14C5 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
cAMP-Dependent Protein Kinase (PKA) (Bos taurus (bovine)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | 25 |
DCR&T, Lilly Spain S.A. | Assay Description In vitro kinase assay using purified enzyme, was incubated at room temperature with substrate, and test compounds in the presence of ATP/[gamma-33P]A... | Bioorg Med Chem Lett 13: 3841-6 (2003) Article DOI: 10.1016/S0960-894X(03)00792-3 BindingDB Entry DOI: 10.7270/Q2FN14C5 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Epidermal growth factor receptor (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | >5.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Ciba-Geigy Limited Curated by ChEMBL | Assay Description Inhibitory activity against recombinant tyrosine kinase EGF-R (EGF-R ICD) | J Med Chem 37: 1015-27 (1994) BindingDB Entry DOI: 10.7270/Q2M32TTP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Cyclic AMP-dependent protein kinase (PKA) (Oryctolagus cuniculus (Rabbit)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB KEGG UniProtKB/TrEMBL B.MOAD GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 2.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Ciba-Geigy Limited Curated by ChEMBL | Assay Description Inhibitory activity was determined against protein kinase A (PKA) of rabbit | J Med Chem 37: 1015-27 (1994) BindingDB Entry DOI: 10.7270/Q2M32TTP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Tyrosine-protein kinase ABL (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Ciba-Geigy Limited Curated by ChEMBL | Assay Description Inhibitory activity against v-abl tyrosine kinase | J Med Chem 37: 1015-27 (1994) BindingDB Entry DOI: 10.7270/Q2M32TTP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Serine/threonine-protein kinase pim-1 (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | 27 | n/a | n/a | n/a | n/a | n/a |
Oxford University Curated by ChEMBL | Assay Description Binding affinity to non phosphorylated PIM1 | J Med Chem 48: 7604-14 (2005) Article DOI: 10.1021/jm0504858 BindingDB Entry DOI: 10.7270/Q2Q52R4H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
PKC alpha and beta-2 (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 212 | n/a | n/a | n/a | n/a | n/a | n/a |
Central Pharmaceutical Research Institute Curated by ChEMBL | Assay Description Inhibitory concentration against recombinant human Protein kinase C beta 2 | Bioorg Med Chem Lett 14: 5171-4 (2004) Article DOI: 10.1016/j.bmcl.2004.07.061 BindingDB Entry DOI: 10.7270/Q2K35VDJ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Protein kinase C alpha type (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 1.60E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Central Pharmaceutical Research Institute Curated by ChEMBL | Assay Description Inhibitory concentration against recombinant human Protein kinase C alpha | Bioorg Med Chem Lett 14: 5171-4 (2004) Article DOI: 10.1016/j.bmcl.2004.07.061 BindingDB Entry DOI: 10.7270/Q2K35VDJ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
NAD-dependent deacetylase sirtuin 2 (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB NCI pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 4.70E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Albert-Ludwigs-Universität Freiburg Curated by ChEMBL | Assay Description Inhibition of human recombinant SIRT2 | J Med Chem 49: 7307-16 (2006) Article DOI: 10.1021/jm060118b BindingDB Entry DOI: 10.7270/Q2TQ616P | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
PKC alpha and beta-2 (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 304 | n/a | n/a | n/a | n/a | n/a | n/a |
Central Pharmaceutical Research Institute Curated by ChEMBL | Assay Description Inhibitory concentration against recombinant human Protein kinase C beta 1 | Bioorg Med Chem Lett 14: 5171-4 (2004) Article DOI: 10.1016/j.bmcl.2004.07.061 BindingDB Entry DOI: 10.7270/Q2K35VDJ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Protein kinase C, epsilon (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 7.52E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Central Pharmaceutical Research Institute Curated by ChEMBL | Assay Description Inhibitory concentration against recombinant human Protein kinase C epsilon | Bioorg Med Chem Lett 14: 5171-4 (2004) Article DOI: 10.1016/j.bmcl.2004.07.061 BindingDB Entry DOI: 10.7270/Q2K35VDJ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Calcium/calmodulin-dependent protein kinase type II subunit delta (Homo sapiens (Human)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 1.19E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Scios, Inc. Curated by ChEMBL | Assay Description Inhibition of CaMK2delta | Bioorg Med Chem Lett 18: 2395-8 (2008) Article DOI: 10.1016/j.bmcl.2008.02.058 BindingDB Entry DOI: 10.7270/Q2QZ2BVW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
cAMP-Dependent Protein Kinase (PKA) (Bos taurus (bovine)) | BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 1.18E+4 | n/a | n/a | n/a | n/a | 8.5 | 37 |
Roche Products Limited | Assay Description The activity of PKA, activated by cAMP, is measured by its ability to transfer phosphate from [gamma-32P]ATP to histone. | J Med Chem 35: 177-84 (1992) Article DOI: 10.1021/jm00079a024 BindingDB Entry DOI: 10.7270/Q2K64G8V | |||||||||||
More data for this Ligand-Target Pair |
Cell (A) | Syringe (B) | Cell Links | Syringe Links | Cell + Syr Links | ΔG° kcal/mole | -TΔS° kcal/mole | ΔH° kcal/mole | log K | pH | Temp °C |
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BDBM2583 (3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(...) | Serine/threonine-protein kinase PIM (Homo sapiens (Human)) | PC cid PC sid | DrugBank GoogleScholar KEGG PDB | -9.78 | 0.548 | -10.4 | 7.57 | 7.5 | 10 | |
Oxford University | J Med Chem 48: 7604-14 (2005) |