BindingDB PrimarySearch

BDBM188517 PF-CBP1

SMILES: CCCOc1ccc(CCc2nc3cc(ccc3n2CCN2CCOCC2)-c2c(C)noc2C)cc1

InChI Key: InChIKey=CGWBJJZOKGZCSJ-UHFFFAOYSA-N

Data: 8 IC50 2 Kd 1 EC50

PDB links: 1 PDB ID matches this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 11 hits for monomerid = 188517
Target/Host (Institution)	Ligand	Target/Host Links	Ligand Links	Trg + Lig Links	Ki nM	ΔG° kcal/mole	IC50 nM	Kd nM	EC50/IC50 nM	k_off s^-1	k_on M^-1s^-1	pH	Temp °C
CREB-binding protein (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	130	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description The assay used His-tagged CBP protein, biotinylated histone H4, and detection reagents europium-labeled streptavidin and anti-6His antibody labeled w...				Chem Biol 22: 1588-96 (2015) Article DOI: 10.1016/j.chembiol.2015.10.013 BindingDB Entry DOI: 10.7270/Q2V69HC0
Pfizer					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	1.81E+4	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description The assay used a Cy5 dye-labeled BRD inhibitor PFI-411FP. The synthesis of the probe and the procedure for the assay was reported recently (Hett et a...				Chem Biol 22: 1588-96 (2015) Article DOI: 10.1016/j.chembiol.2015.10.013 BindingDB Entry DOI: 10.7270/Q2V69HC0
Pfizer					More data for this Ligand-Target Pair
CREB-binding protein (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	n/a	190	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).				Chem Biol 22: 1588-96 (2015) Article DOI: 10.1016/j.chembiol.2015.10.013 BindingDB Entry DOI: 10.7270/Q2V69HC0
Pfizer					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	n/a	>2.00E+4	n/a	n/a	n/a	n/a	n/a
Pfizer					Assay Description Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).				Chem Biol 22: 1588-96 (2015) Article DOI: 10.1016/j.chembiol.2015.10.013 BindingDB Entry DOI: 10.7270/Q2V69HC0
Pfizer					More data for this Ligand-Target Pair
CREB-binding protein (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	190	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
Genentech Curated by ChEMBL					More data for this Ligand-Target Pair
CREB-binding protein (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	130	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer Inc. Curated by ChEMBL					Assay Description Inhibition of CREBBP (unknown origin) by FRET assay				J Med Chem 60: 5349-5363 (2017) Article DOI: 10.1021/acs.jmedchem.6b01839 BindingDB Entry DOI: 10.7270/Q2B85BCF
Pfizer Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
CREB-binding protein (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	>1.00E+4	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 NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incuba...				J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF
Genentech Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	2.90E+3	n/a	n/a	n/a	n/a	n/a	n/a
Genentech Curated by ChEMBL					Assay Description Displacement of biotinylated ligand from BRD4 bromodomain-1 (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
Genentech Curated by ChEMBL					More data for this Ligand-Target Pair
Bromodomain-containing protein 4 (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	1.81E+4	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer Inc. Curated by ChEMBL					Assay Description Inhibition of BRD4 (unknown origin) by fluorescence polarization assay				J Med Chem 60: 5349-5363 (2017) Article DOI: 10.1021/acs.jmedchem.6b01839 BindingDB Entry DOI: 10.7270/Q2B85BCF
Pfizer Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Alpha-1A adrenergic receptor (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	620	n/a	n/a	n/a	n/a	n/a	n/a
Pfizer Inc. Curated by ChEMBL					Assay Description Displacement of [3H]prazosin from recombinant human adrenergic A1a receptor after 60 mins by scintillation counting method				J Med Chem 60: 5349-5363 (2017) Article DOI: 10.1021/acs.jmedchem.6b01839 BindingDB Entry DOI: 10.7270/Q2B85BCF
Pfizer Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
CREB-binding protein/Histone acetyltransferase p300 (Homo sapiens (Human))	BDBM188517 (PF-CBP1) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid PDB UniChem Similars	Article PubMed	n/a	n/a	n/a	n/a	6.60E+3	n/a	n/a	n/a	n/a
Genentech Curated by ChEMBL					Assay Description Inhibition of CBP/EP300 (unknown origin) assessed as reduction in MYC expression by cell based assay				J Med Chem 59: 10549-10563 (2016) Article DOI: 10.1021/acs.jmedchem.6b01022 BindingDB Entry DOI: 10.7270/Q27083DF
Genentech Curated by ChEMBL					More data for this Ligand-Target Pair