bromodomain and PHD finger containing 1 | Non-enzymatic BRD containing proteins | IUPHAR/BPS Guide to PHARMACOLOGY

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bromodomain and PHD finger containing 1

Target not currently curated in GtoImmuPdb

Target id: 2730

Nomenclature: bromodomain and PHD finger containing 1

Family: Non-enzymatic BRD containing proteins

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1220 3p26-p25 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
BR140 | peregrin | bromodomain and PHD finger containing, 1 | bromodomain and PHD finger containing
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
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 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 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 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] Hs Binding 6.9 pKd 1
pKd 6.9 (Kd 1.37x10-7 M) [1]
compound 2 [PMID: 25408830] Hs Binding 5.6 pIC50 2
pIC50 5.6 (IC50 2.511x10-6 M) [2]
compound 1 [PMID: 25408830] Hs Binding 5.0 pIC50 2
pIC50 5.0 (IC50 1x10-5 M) [2]
compound 3 [PMID: 25408830] 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 19/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2730.