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FKBP prolyl isomerase 5

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Target not currently curated in GtoImmuPdb

Target id: 3175

Nomenclature: FKBP prolyl isomerase 5

Abbreviated Name: FKBP51

Family: Peptidyl-prolyl cis/trans isomerases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 457 6p21.31 FKBP5 FKBP prolyl isomerase 5
Mouse - 456 Ch17, 14.66 cM Fkbp5 FK506 binding protein 5
Rat - 456 20p12 Fkbp5 FKBP prolyl isomerase 5
Previous and Unofficial Names Click here for help
FKBP51 | FKBP-51 | Ptg-10
Database Links Click here for help
Alphafold Q13451 (Hs), Q64378 (Mm)
BRENDA 5.2.1.8
ChEMBL Target CHEMBL2052031 (Hs), CHEMBL3792270 (Mm)
Ensembl Gene ENSG00000096060 (Hs), ENSMUSG00000024222 (Mm), ENSRNOG00000022523 (Rn)
Entrez Gene 2289 (Hs), 14229 (Mm), 361810 (Rn)
Human Protein Atlas ENSG00000096060 (Hs)
KEGG Enzyme 5.2.1.8
KEGG Gene hsa:2289 (Hs), mmu:14229 (Mm), rno:361810 (Rn)
OMIM 602623 (Hs)
Pharos Q13451 (Hs)
RefSeq Nucleotide NM_001145775 (Hs), NM_010220 (Mm), NM_001012174 (Rn)
RefSeq Protein NP_001139247 (Hs), NP_034350 (Mm), NP_001012174 (Rn)
UniProtKB Q13451 (Hs), Q64378 (Mm)
Wikipedia FKBP5 (Hs)
Enzyme Reaction Click here for help
EC Number: 5.2.1.8

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SAFit1 Small molecule or natural product Ligand has a PDB structure Hs - 8.4 pKi 1
⤷ pKi 8.4 (Ki 4x10-9 M) [1]
SAFit2 Small molecule or natural product Hs - 8.2 pKi 1
⤷ pKi 8.2 (Ki 6x10-9 M) [1]
compound 19b [PMID: 37058391] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pKi 3
⤷ pKi 7.7 (Ki 1.9x10-8 M) [3]
SLF Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - 5.2 pIC50 2
⤷ pIC50 5.2 (IC50 6.3x10-6 M) [2]
Description: Binding affinity determined by a fluorescence polarization assay

References

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1. Gaali S, Kirschner A, Cuboni S, Hartmann J, Kozany C, Balsevich G, Namendorf C, Fernandez-Vizarra P, Sippel C, Zannas AS et al.. (2015) Selective inhibitors of the FK506-binding protein 51 by induced fit. Nat Chem Biol, 11 (1): 33-7. [PMID:25436518]

2. Gopalakrishnan R, Kozany C, Wang Y, Schneider S, Hoogeland B, Bracher A, Hausch F. (2012) Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52. J Med Chem, 55 (9): 4123-31. [PMID:22455398]

3. Knaup FH, Meyners C, Sugiarto WO, Wedel S, Springer M, Walz C, Geiger TM, Schmidt M, Sisignano M, Hausch F. (2023) Structure-Based Discovery of a New Selectivity-Enabling Motif for the FK506-Binding Protein 51. J Med Chem, 66 (8): 5965-5980. [PMID:37058391]

Contributors

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