BDBM50200384 CHEMBL3968533::US9763922, Example 299
SMILES: CC(=O)N1CCc2c(C1)c(Nc1ccc(cc1F)-c1cnn(C)c1)nn2[C@@H]1CCOC1
InChI Key: InChIKey=NKOJNOBJGYTLLZ-QGZVFWFLSA-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 |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
CREB-binding protein (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 20 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from CBP (unknown origin) by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 6.25E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC. US Patent | Assay Description His/Flag epitope tagged BRD4 BD142-168 was cloned, expressed, and purified to. BRD4 binding and inhibition was assessed by monitoring the engagement ... | US Patent US9763922 (2017) BindingDB Entry DOI: 10.7270/Q23N25G6 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BRD4 bromodomain-1 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Bromodomain-containing protein 8 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | UniProtKB/SwissProt GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BRD8 bromodomain-1 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone acetyltransferase KAT2A/KAT2B (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged PCAF (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
CREB-binding protein/Histone acetyltransferase p300 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB UniProtKB/SwissProt antibodypedia antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 400 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Inhibition of Halo-tagged histone H3.3 binding to CBP/EP300 (unknown origin) expressed in HEK293 cells measured after overnight incubation by lucifer... | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
CREB-binding protein/Histone acetyltransferase p300 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB UniProtKB/SwissProt antibodypedia antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 69 | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Inhibition of CBP/EP300 in human MOLM16 cells assessed as decrease in MYC expression measured after 4 hrs by RT-PCR analysis | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone acetyltransferase p300/Hypoxia-inducible factor 1-alpha (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB MMDB UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 30 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged EP300 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Nucleosome-remodeling factor subunit BPTF (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BPTF (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Peregrin (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BRPF1 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Transcription initiation factor TFIID subunit 1 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 1.20E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged TAF1 bromodomain 2 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Bromodomain adjacent to zinc finger domain protein 2B (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BAZ2B (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Bromodomain-containing protein 9 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BRD9 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Transcription initiation factor TFIID subunit 1 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged TAF1 bromodomain 1 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
CREB-binding protein/Histone acetyltransferase p300 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB UniProtKB/SwissProt antibodypedia antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 910 | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Inhibition of CBP/EP300 in human MV4-11 cells assessed as inhibition of MYC expression measured after 4 hrs by luminescence analysis | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Cat eye syndrome critical region protein 2 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged CECR2 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 1.30E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged BRD4 bromodomain-1 (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
CREB-binding protein (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 40 | n/a | n/a | n/a | n/a | n/a | n/a |
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC. US Patent | Assay Description His/Flag epitope tagged CBP was cloned, expressed, and purified to homogeneity. CBP binding and inhibition was assessed by monitoring the engagement ... | US Patent US9763922 (2017) BindingDB Entry DOI: 10.7270/Q23N25G6 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone acetyltransferase KAT2A (Homo sapiens (Human)) | BDBM50200384 (CHEMBL3968533 | US9763922, Example 299) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | CHEMBL PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Curated by ChEMBL | Assay Description Displacement of biotinylated ligand from recombinant His-tagged GCN5 long isoform (unknown origin) measured after 10 mins by TR-FRET assay | J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF | |||||||||||
More data for this Ligand-Target Pair |