apstatin [Ligand Id: 8803] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL311875
  • Leucine aminopeptidase 3/Leucine aminopeptidase in Human [ChEMBL: CHEMBL3965] [GtoPdb: 1569] [UniProtKB: P28838]
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  • X-prolyl aminopeptidase 1/Xaa-Pro aminopeptidase 1 in Human [ChEMBL: CHEMBL3782] [GtoPdb: 1578] [UniProtKB: Q9NQW7]
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  • X-prolyl aminopeptidase 2/Xaa-Pro aminopeptidase 2 in Human [ChEMBL: CHEMBL4610] [GtoPdb: 1579] [UniProtKB: O43895]
  • X-prolyl aminopeptidase 2/Xaa-Pro aminopeptidase 2 in Rat [ChEMBL: CHEMBL2970] [GtoPdb: 1579] [UniProtKB: Q99MA2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Leucine aminopeptidase 3/Leucine aminopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3965] [GtoPdb: 1569] [UniProtKB: P28838]
ChEMBL Inhibition against Leucyl aminopeptidase from pig kidney. B 6.52 pIC50 300 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]
X-prolyl aminopeptidase 1/Xaa-Pro aminopeptidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3782] [GtoPdb: 1578] [UniProtKB: Q9NQW7]
ChEMBL Inhibition against cytosolic Aminopeptidase P from human heart. B 4.68 pIC50 21000 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]
GtoPdb - - 4.68 pIC50 21000 nM IC50 J Med Chem (1999) 42: 2394-402 [PMID:10395480]
ChEMBL Inhibition against Aminopeptidase P from human platelets. B 4.74 pIC50 18000 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]
ChEMBL Inhibition of 6-His tagged XPNPEP1 (unknown origin) expressed in Escherichia coli Rosetta DE3 cells using H-Lys(abz)-Pro-Pro-pNA as substrate incubated for 60 mins by fluorescence based analysis B 4.74 pIC50 18000 nM IC50 J Med Chem (2023) 66: 2589-2607 [PMID:36724486]
X-prolyl aminopeptidase 2/Xaa-Pro aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4610] [GtoPdb: 1579] [UniProtKB: O43895]
GtoPdb - - 6.19 pKi 640 nM Ki J Med Chem (1999) 42: 2394-402 [PMID:10395480]
ChEMBL Inhibition against membrane bound monkey aminopeptidase P B 5.21 pIC50 6100 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]
ChEMBL Inhibition against membrane bound human aminopeptidase P B 5.54 pIC50 2900 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]
GtoPdb - - 5.54 pIC50 2900 nM IC50 J Med Chem (1999) 42: 2394-402 [PMID:10395480]
X-prolyl aminopeptidase 2/Xaa-Pro aminopeptidase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2970] [GtoPdb: 1579] [UniProtKB: Q99MA2]
ChEMBL Activity against membrane bound rat aminopeptidase P B 5.39 pIC50 4100 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]
peptidase D/Xaa-Pro dipeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4185] [GtoPdb: 2389] [UniProtKB: P12955]
ChEMBL Inhibition of recombinant human PEPD using Ala-Pro as substrate assessed as alanine release by measuring increase in fluorescense signal by fluorescence based analysis B 4.59 pIC50 26000 nM IC50 J Med Chem (2023) 66: 2589-2607 [PMID:36724486]
ChEMBL Inhibition against Prolidase from pig kidney. B 5.31 pIC50 4900 nM IC50 J Med Chem (1999) 42: 2394-2402 [PMID:10395480]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]