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bromodomain and PHD finger containing 1

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Target not currently curated in GtoImmuPdb

Target id: 2730

Nomenclature: bromodomain and PHD finger containing 1

Family: Non-enzymatic BRD containing proteins

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1214 3p25.3 BRPF1 bromodomain and PHD finger containing 1
Mouse - 1247 6 E3 Brpf1 bromodomain and PHD finger containing, 1
Rat - 1246 4q42 Brpf1 bromodomain and PHD finger containing, 1
Previous and Unofficial Names Click here for help
BR140 | peregrin | bromodomain and PHD finger containing, 1 | bromodomain and PHD finger containing
Database Links Click here for help
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  X-ray structure of the bromodomain of human BRPF1 with the small molecule inhibitor N-1,3-dimethyl-2-oxo-6-(piperidin-1- yl)-2,3-dihydro-1H-1,3-benzodiazol-5-yl-2-methoxybenzamide
PDB Id:  4UYE
Ligand:  compound 3 [PMID: 25408830]
Resolution:  1.65Å
Species:  Human
References:  2
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PFI-4 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Binding 7.9 pKd 5
pKd 7.9 (Kd 1.3x10-8 M) [5]
Description: Isothermal titration calorimetry (ITC) assay measuring binding to the BRPF1B isoform.
NI-57 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Binding 7.5 pKd 4
pKd 7.5 (Kd 3.1x10-8 M) [4]
Description: Isothermal titration calorimetry (ITC) assay, measuring binding to BRPF1B isoform.
OF-1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Binding 7.0 pKd 3
pKd 7.0 (Kd 1x10-7 M) [3]
Description: By isothermal titration calorimetry, using the BRPF1B isoform.
compound 34 [PMID: 25974391] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Binding 6.9 pKd 1
pKd 6.9 (Kd 1.37x10-7 M) [1]
compound 2 [PMID: 25408830] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Binding 5.6 pIC50 2
pIC50 5.6 (IC50 2.511x10-6 M) [2]
compound 1 [PMID: 25408830] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Binding 5.0 pIC50 2
pIC50 5.0 (IC50 1x10-5 M) [2]
compound 3 [PMID: 25408830] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Binding <4.3 pIC50 2
pIC50 <4.3 (IC50 >5.012x10-5 M) [2]

References

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1. Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C et al.. (2016) Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. J. Med. Chem., 59 (4): 1642-7. [PMID:25974391]

2. Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ et al.. (2014) 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett, 5 (11): 1190-1195. [PMID:25408830]

3. SGC. OF-1 A chemical probe for BRPF bromodomains. Accessed on 05/04/2017. Modified on 05/04/2017. SGC, http://www.thesgc.org/chemical-probes/OF-1

4. Structural Genomics Consortium. NI-57 – a chemical probe for BRPF bromodomains. Accessed on 15/07/2015. Modified on 15/07/2015. http://www.thesgc.org, http://www.thesgc.org/chemical-probes/NI-57

5. Structural Genomics Consortium. PFI-4- a chemical probe for BRPF1B. Accessed on 15/07/2015. Modified on 15/07/2015. http://www.thesgc.org, http://www.thesgc.org/chemical-probes/PFI-4

How to cite this page

Non-enzymatic BRD containing proteins: bromodomain and PHD finger containing 1. Last modified on 05/04/2017. Accessed on 05/12/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2730.