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Target
Leucyl-cystinyl aminopeptidase
Ligand
BDBM50245402
Substrate
n/a
Meas. Tech.
ChEMBL_1674664 (CHEMBL4024807)
IC50
46±n/a nM
Citation
 Kokkala, P; Mpakali, A; Mauvais, FX; Papakyriakou, A; Daskalaki, I; Petropoulou, I; Kavvalou, S; Papathanasopoulou, M; Agrotis, S; Fonsou, TM; van Endert, P; Stratikos, E; Georgiadis, D Optimization and Structure-Activity Relationships of Phosphinic Pseudotripeptide Inhibitors of Aminopeptidases That Generate Antigenic Peptides. J Med Chem 59:9107-9123 (2016) [PubMed]  Article 
Target
Name:
Leucyl-cystinyl aminopeptidase
Synonyms:
Aminopeptidase | Aminopeptidase (P-LAP) | Cystinyl aminopeptidase | IRAP | Insulin-regulated membrane aminopeptidase | Insulin-responsive aminopeptidase | LCAP_HUMAN | LNPEP | Leucyl-cystinyl aminopeptidase, pregnancy serum form | OTASE | Oxytocinase | P-LAP | Placental leucine aminopeptidase
Type:
PROTEIN
Mol. Mass.:
117334.10
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1473494
Residue:
1025
Sequence:
MEPFTNDRLQLPRNMIENSMFEEEPDVVDLAKEPCLHPLEPDEVEYEPRGSRLLVRGLGEHEMEEDEEDYESSAKLLGMSFMNRSSGLRNSATGYRQSPDGACSVPSARTMVVCAFVIVVAVSVIMVIYLLPRCTFTKEGCHKKNQSIGLIQPFATNGKLFPWAQIRLPTAVVPLRYELSLHPNLTSMTFRGSVTISVQALQVTWNIILHSTGHNISRVTFMSAVSSQEKQAEILEYAYHGQIAIVAPEALLAGHNYTLKIEYSANISSSYYGFYGFSYTDESNEKKYFAATQFEPLAARSAFPCFDEPAFKATFIIKIIRDEQYTALSNMPKKSSVVLDDGLVQDEFSESVKMSTYLVAFIVGEMKNLSQDVNGTLVSIYAVPEKIGQVHYALETTVKLLEFFQNYFEIQYPLKKLDLVAIPDFEAGAMENWGLLTFREETLLYDSNTSSMADRKLVTKIIAHELAHQWFGNLVTMKWWNDLWLNEGFATFMEYFSLEKIFKELSSYEDFLDARFKTMKKDSLNSSHPISSSVQSSEQIEEMFDSLSYFKGSSLLLMLKTYLSEDVFQHAVVLYLHNHSYASIQSDDLWDSFNEVTNQTLDVKRMMKTWTLQKGFPLVTVQKKGKELFIQQERFFLNMKPEIQPSDTSYLWHIPLSYVTEGRNYSKYQSVSLLDKKSGVINLTEEVLWVKVNINMNGYYIVHYADDDWEALIHQLKINPYVLSDKDRANLINNIFELAGLGKVPLKRAFDLINYLGNENHTAPITEALFQTDLIYNLLEKLGYMDLASRLVTRVFKLLQNQIQQQTWTDEGTPSMRELRSALLEFACTHNLGNCSTTAMKLFDDWMASNGTQSLPTDVMTTVFKVGAKTDKGWSFLLGKYISIGSEAEKNKILEALASSEDVRKLYWLMKSSLNGDNFRTQKLSFIIRTVGRHFPGHLLAWDFVKENWNKLVQKFPLGSYTIQNIVAGSTYLFSTKTHLSEVQAFFENQSEATFRLRCVQEALEVIQLNIQWMEKNLKSLTWWL
  
Inhibitor
Name:
BDBM50245402
Synonyms:
CHEMBL4074464
Type:
Small organic molecule
Emp. Form.:
C32H44N3O4P
Mol. Mass.:
565.6832
SMILES:
N[C@@H](CCc1ccccc1)P(O)(=O)C[C@@H](CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |r,THB:21:22:19.20.25:17,21:20:17:23.22.24,15:16:19:23.22.21,24:22:19:25.16.17,24:16:19:23.22.21|
Structure:
Search PDB for entries with ligand similarity: