bromodomain and PHD finger containing 1

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

   GtoImmuPdb view: OFF :     Currently no data for bromodomain and PHD finger containing 1 in GtoImmuPdb

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
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 Affinity Units 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 18/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2730.