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bromodomain and PHD finger containing 1

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Target id: 2730

Nomenclature: bromodomain and PHD finger containing 1

Family: Non-enzymatic BRD containing proteins

Contents:

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
Alphafold P55201 (Hs)
CATH/Gene3D 1.20.920.10, 3.30.40.10
ChEMBL Target CHEMBL3132741 (Hs)
Ensembl Gene ENSG00000156983 (Hs), ENSMUSG00000001632 (Mm), ENSRNOG00000008142 (Rn)
Entrez Gene 7862 (Hs), 78783 (Mm), 679713 (Rn)
Human Protein Atlas ENSG00000156983 (Hs)
KEGG Gene hsa:7862 (Hs), mmu:78783 (Mm), rno:679713 (Rn)
OMIM 602410 (Hs)
Pharos P55201 (Hs)
RefSeq Nucleotide NM_001003694 (Hs), NM_001282126 (Mm), NM_001191572 (Rn)
RefSeq Protein NP_001003694 (Hs), NP_001269055 (Mm), NP_001178501 (Rn)
SynPHARM 80630 (in complex with compound 3 [PMID: 25408830])
84275 (in complex with OF-1)
82372 (in complex with PFI-4)
UniProtKB P55201 (Hs)
Wikipedia BRPF1 (Hs)
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 3
⤷ pKd 7.5 (Kd 3.1x10-8 M) [3]
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 4
⤷ pKd 7.0 (Kd 1x10-7 M) [4]
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. NI-57 – a chemical probe for BRPF bromodomains. Accessed on 15/07/2015. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/NI-57

4. SGC. OF-1 A chemical probe for BRPF bromodomains. Accessed on 05/04/2017. Modified on 04/08/2023. SGC, https://www.thesgc.org/chemical-probes/OF-1

5. SGC. PFI-4 A chemical probe for BRPF1B. Accessed on 15/07/2015. Modified on 04/08/2023. thesgc.org, https://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 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2730.