BDBM188519 SGC-CBP30
SMILES COc1ccc(CCc2nc3cc(ccc3n2C[C@H](C)N2CCOCC2)-c2c(C)noc2C)cc1Cl
InChI Key InChIKey=GEPYBHCJBORHCE-SFHVURJKSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 38 hits for monomerid = 188519
Affinity DataKd: 21nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: 67nMAssay Description:Inhibition of EP300 bromodomain (unknown origin) incubated for 20 mins by AlphaLISA methodMore data for this Ligand-Target Pair
Affinity DataKd: 32nMAssay Description:Binding affinity to human p300 by ITC analysisMore data for this Ligand-Target Pair
Affinity DataKd: 21nMAssay Description:Binding affinity to human CBP by ITC analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.50E+3nMAssay Description:Inhibition of doxorubicin-stimulated p53 (unknown origin) expressed in human RKO cells preincubated for 24 hrs followed by addition of doxorubicin fo...More data for this Ligand-Target Pair
Affinity DataIC50: 69nMAssay Description:Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged CBP by alphascreen assayMore data for this Ligand-Target Pair
Affinity DataKd: 21nMAssay Description:Binding affinity to human CBP by isothermal titration calorimetric analysisMore data for this Ligand-Target Pair
TargetCREB-binding protein/Histone acetyltransferase p300(Homo sapiens (Human))
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataEC50: 6.90E+3nMAssay Description:Inhibition of CBP/EP300 (unknown origin) assessed as reduction in MYC expression by cell based assayMore data for this Ligand-Target Pair
TargetCREB-binding protein/Histone acetyltransferase p300(Homo sapiens (Human))
Genentech
Curated by ChEMBL
Genentech
Curated by ChEMBL
Affinity DataKd: 21nMAssay Description:Binding affinity to human N-terminal His10-tagged/C-terminal Biotin-tagged CBP (R1081 to G1198 residues)/P300 expressed in Escherichia coli BL21(DE3)...More data for this Ligand-Target Pair
Affinity DataIC50: 2.80E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incuba...More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Displacement of biotinylated ligand from CBP (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.20E+3nMAssay Description:Displacement of biotinylated ligand from BRD4 bromodomain-1 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.85E+3nMAssay Description:Inhibition of human BRD4 by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 64nMAssay Description:Inhibition of human CREBBP by FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 79nMAssay Description:Inhibition of human CREBBP by AlphaScreen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 125nMAssay Description:Inhibition of His6-tagged human CREBBP (R1081 to G1197 residues) expressed in Escherichia coli BL21(DE3) using biotinylated-H4KAc4 as substrate by Al...More data for this Ligand-Target Pair
TargetHistone acetyltransferase KAT2B(Homo sapiens (Human))
Guangzhou Medical University
Curated by ChEMBL
Guangzhou Medical University
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged PCAF (G715 to D831 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs by ...More data for this Ligand-Target Pair
TargetTranscription initiation factor TFIID subunit 1(Homo sapiens (Human))
Guangzhou Medical University
Curated by ChEMBL
Guangzhou Medical University
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged TAF-1 (R1377 to D1503 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs ...More data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged EP300 (A1040 to G1161 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs ...More data for this Ligand-Target Pair
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged BRD4 bromodomain-1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) afte...More data for this Ligand-Target Pair
TargetBromodomain adjacent to zinc finger domain protein 2B(Homo sapiens (Human))
Guangzhou Medical University
Curated by ChEMBL
Guangzhou Medical University
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged BAZ2B (S1858 to S1972 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 9(Homo sapiens (Human))
Guangzhou Medical University
Curated by ChEMBL
Guangzhou Medical University
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged BRD9 (L14 to Q134 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs by l...More data for this Ligand-Target Pair
TargetTranscription intermediary factor 1-alpha(Homo sapiens (Human))
Guangzhou Medical University
Curated by ChEMBL
Guangzhou Medical University
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged TIF-1 (G896 to E1014 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs b...More data for this Ligand-Target Pair
Affinity DataIC50: 80nMAssay Description:Inhibition of biotinylated-H4KAc4 binding to human His6-tagged CBP (R1081 to G1197 residues) expressed in Escherichia coli BL21(DE3) after 2.5 hrs by...More data for this Ligand-Target Pair
Affinity DataIC50: 2.78E+4nMAssay Description:Inhibition of human BRD4 BD1 (67 to 152 residues) preincubated for 15 mins followed by addition of C-terminal biotinylated synthetic K5,8,12,16 tetra...More data for this Ligand-Target Pair
Affinity DataIC50: 7.12E+3nMAssay Description:Inhibition of human BRD4 BD1 (67 to 152 residues) preincubated for 15 mins followed by addition of C-terminal biotinylated synthetic K5,8,12,16 tetra...More data for this Ligand-Target Pair
Affinity DataIC50: 68nMAssay Description:Inhibition of human BRD4 BD1 (67 to 152 residues) preincubated for 15 mins followed by addition of C-terminal biotinylated synthetic K5,8,12,16 tetra...More data for this Ligand-Target Pair
Affinity DataIC50: 66nMAssay Description:Inhibition of human BRD4 BD1 (67 to 152 residues) preincubated for 15 mins followed by addition of C-terminal biotinylated synthetic K5,8,12,16 tetra...More data for this Ligand-Target Pair
Affinity DataKd: 3.18E+7nMAssay Description:Inhibition of human BRD4 BD1 (67 to 152 residues) preincubated for 15 mins followed by addition of C-terminal biotinylated synthetic K5,8,12,16 tetra...More data for this Ligand-Target Pair
Affinity DataKd: 21nMAssay Description:Binding affinity to human CBP by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 850nMAssay Description:Binding affinity to human BRD4 bromodomain1 by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 5.20E+3nMAssay Description:Binding affinity to human BRD4 bromodomain2 by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 21nMAssay Description:Binding affinity to human CBP measured at 15 degreeC by ITC assayMore data for this Ligand-Target Pair
Affinity DataIC50: 64nMAssay Description:Inhibition of human CBP by FRET assayMore data for this Ligand-Target Pair
Affinity DataKd: 850nMAssay Description:Binding affinity to human BRD4 measured at 15 degreeC by ITC assayMore data for this Ligand-Target Pair
Affinity DataIC50: 28nMAssay Description:Inhibition of His-tagged CBP (unknown origin) using biotinylated-H3K56ac peptide as substrate incubated for 1 hr by AlphaScreen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 7.94E+3nMAssay Description:Inhibition of His-tagged BRD4 BD1 (unknown origin) using biotinylated-JQ1 peptide as substrate incubated for 1 hr by AlphaScreen assayMore data for this Ligand-Target Pair
Affinity DataKd: 850nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair