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bromodomain adjacent to zinc finger domain 2B

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Target id: 2722

Nomenclature: bromodomain adjacent to zinc finger domain 2B

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 - 2168 2q24.2 BAZ2B bromodomain adjacent to zinc finger domain 2B
Mouse - 2123 2 C1.1 Baz2b bromodomain adjacent to zinc finger domain, 2B
Rat - 2191 3q21 Baz2b bromodomain adjacent to zinc finger domain, 2B
Previous and Unofficial Names Click here for help
WALp4 | bromodomain adjacent to zinc finger domain, 2B | bromodomain adjacent to zinc finger domain
Database Links Click here for help
Alphafold Q9UIF8 (Hs)
CATH/Gene3D 1.20.920.10, 3.30.40.10
ChEMBL Target CHEMBL1741220 (Hs)
Ensembl Gene ENSG00000123636 (Hs), ENSMUSG00000026987 (Mm), ENSRNOG00000056984 (Rn)
Entrez Gene 29994 (Hs), 407823 (Mm), 317627 (Rn)
Human Protein Atlas ENSG00000123636 (Hs)
KEGG Gene hsa:29994 (Hs), mmu:407823 (Mm), rno:317627 (Rn)
OMIM 605683 (Hs)
Pharos Q9UIF8 (Hs)
RefSeq Nucleotide NM_013450 (Hs), NM_001001182 (Mm), NM_001108260 (Rn)
RefSeq Protein NP_038478 (Hs), NP_001001182 (Mm), NP_001101730 (Rn)
SynPHARM 81939 (in complex with compound 1 [PMID: 25719566])
81941 (in complex with compound 7 [PMID: 25719566])
81847 (in complex with GSK2801)
UniProtKB Q9UIF8 (Hs)
Wikipedia BAZ2B (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the bromodomain of human BAZ2B in complex WITH GSK2801
PDB Id:  4RVR
Ligand:  GSK2801
Resolution:  1.98Å
Species:  Human
References: 
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the bromodomain of human BAZ2B in complex with E11919 BAZ2-ICR analogue
PDB Id:  4XUA
Ligand:  compound 1 [PMID: 25719566]
Resolution:  1.75Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the bromodomain of human BAZ2B in complex with BAZ2-ICR chemical probe
PDB Id:  4XUB
Ligand:  compound 7 [PMID: 25719566]
Resolution:  1.98Å
Species:  Human
References:  1

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK2801 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 2
⤷ pKd 6.9 (Kd 1.36x10-7 M) [2]
Description: Isothermal titration calorimetry (ITC) assay
BAZ2-ICR Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pKd 1
⤷ pKd 6.8 (Kd 1.7x10-7 M) [1]
Description: Isothermal titration calorimetry (ITC) assay
compound 7 [PMID: 25719566] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 6.0 pIC50 1
⤷ pIC50 6.0 (IC50 1.1x10-6 M) [1]
compound 1 [PMID: 25719566] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 4.6 pIC50 1
⤷ pIC50 4.6 (IC50 2.6x10-5 M) [1]

References

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1. Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M et al.. (2015) Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B. J Med Chem, 58 (5): 2553-9. [PMID:25719566]

2. SGC. GSK2801: A Selective Chemical Probe for BAZ2B/A bromodomains. Accessed on 03/03/2015. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/GSK2801

How to cite this page

Non-enzymatic BRD containing proteins: bromodomain adjacent to zinc finger domain 2B. Last modified on 29/01/2016. Accessed on 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2722.