Target
Endoplasmic reticulum aminopeptidase 1
Ligand
BDBM50570849
Substrate
n/a
Meas. Tech.
ChEMBL_2113192 (CHEMBL4822042)
IC50
141±n/a nM
Citation
 Wilding, BPasqua, AEE A Chessum, NPierrat, OAHahner, TTomlin, KShehu, EBurke, RRichards, GMWhitton, BArwert, ENThapaliya, ASalimraj, Rvan Montfort, RSkawinska, AHayes, ARaynaud, FChopra, RJones, KNewton, GCheeseman, MD Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1. Bioorg Med Chem Lett 42:0 (2021) [PubMed]  Article 
Target
Name:
Endoplasmic reticulum aminopeptidase 1
Synonyms:
APPILS | ARTS1 | Aminopeptidase | ERAP1 | ERAP1_HUMAN | KIAA0525
Type:
PROTEIN
Mol. Mass.:
107232.03
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1473167
Residue:
941
Sequence:
MVFLPLKWSLATMSFLLSSLLALLTVSTPSWCQSTEASPKRSDGTPFPWNKIRLPEYVIPVHYDLLIHANLTTLTFWGTTKVEITASQPTSTIILHSHHLQISRATLRKGAGERLSEEPLQVLEHPRQEQIALLAPEPLLVGLPYTVVIHYAGNLSETFHGFYKSTYRTKEGELRILASTQFEPTAARMAFPCFDEPAFKASFSIKIRREPRHLAISNMPLVKSVTVAEGLIEDHFDVTVKMSTYLVAFIISDFESVSKITKSGVKVSVYAVPDKINQADYALDAAVTLLEFYEDYFSIPYPLPKQDLAAIPDFQSGAMENWGLTTYRESALLFDAEKSSASSKLGITMTVAHELAHQWFGNLVTMEWWNDLWLNEGFAKFMEFVSVSVTHPELKVGDYFFGKCFDAMEVDALNSSHPVSTPVENPAQIREMFDDVSYDKGACILNMLREYLSADAFKSGIVQYLQKHSYKNTKNEDLWDSMASICPTDGVKGMDGFCSRSQHSSSSSHWHQEGVDVKTMMNTWTLQKGFPLITITVRGRNVHMKQEHYMKGSDGAPDTGYLWHVPLTFITSKSDMVHRFLLKTKTDVLILPEEVEWIKFNVGMNGYYIVHYEDDGWDSLTGLLKGTHTAVSSNDRASLINNAFQLVSIGKLSIEKALDLSLYLKHETEIMPVFQGLNELIPMYKLMEKRDMNEVETQFKAFLIRLLRDLIDKQTWTDEGSVSERMLRSQLLLLACVHNYQPCVQRAEGYFRKWKESNGNLSLPVDVTLAVFAVGAQSTEGWDFLYSKYQFSLSSTEKSQIEFALCRTQNKEKLQWLLDESFKGDKIKTQEFPQILTLIGRNPVGYPLAWQFLRKNWNKLVQKFELGSSSIAHMVMGTTNQFSTRTRLEEVKGFFSSLKENGSQLRCVQQTIETIEENIGWMDKNFDKIRVWLQSEKLERM
  
Inhibitor
Name:
BDBM50570849
Synonyms:
CHEMBL4854733
Type:
Small organic molecule
Emp. Form.:
C28H38N3O5P
Mol. Mass.:
527.5922
SMILES:
COC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)CP(O)(=O)[C@@H](N)CCc1ccccc1 |r|
Structure:
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