Reaction Details Report a problem with these data
Target
Methionine aminopeptidase 1
Ligand
BDBM17594
Substrate
Octapeptide substrate
Meas. Tech.
MetAP Enzyme Activity Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
57000±n/a nM
Citation
Wang, J; Sheppard, GS; Lou, P; Kawai, M; BaMaung, N; Erickson, SA; Tucker-Garcia, L; Park, C; Bouska, J; Wang, YC; Frost, D; Tapang, P; Albert, DH; Morgan, SJ; Morowitz, M; Shusterman, S; Maris, JM; Lesniewski, R; Henkin, J Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2. Cancer Res 63:7861-9 (2003) [PubMed]
More Info.:
Target
Name:
Methionine aminopeptidase 1
Synonyms:
Aminopeptidase | KIAA0094 | MAP 1 | MAP11_HUMAN | METAP1 | MetAP 1 | Methionine Aminopeptidase Type 1 (MetAP1) | Peptidase M 1
Type:
Enzyme
Mol. Mass.:
43220.79
Organism:
Homo sapiens (Human)
Description:
MetAP1 with an N-terminal six histidine tag was expressed in baculovirus infected sf9 cells.
Residue:
386
Sequence:
MAAVETRVCETDGCSSEAKLQCPTCIKLGIQGSYFCSQECFKGSWATHKLLHKKAKDEKAKREVSSWTVEGDINTDPWAGYRYTGKLRPHYPLMPTRPVPSYIQRPDYADHPLGMSESEQALKGTSQIKLLSSEDIEGMRLVCRLAREVLDVAAGMIKPGVTTEEIDHAVHLACIARNCYPSPLNYYNFPKSCCTSVNEVICHGIPDRRPLQEGDIVNVDITLYRNGYHGDLNETFFVGEVDDGARKLVQTTYECLMQAIDAVKPGVRYRELGNIIQKHAQANGFSVVRSYCGHGIHKLFHTAPNVPHYAKNKAVGVMKSGHVFTIEPMICEGGWQDETWPDGWTAVTRDGKRSAQFEHTLLVTDTGCEILTRRLDSARPHFMSQF
Inhibitor
Name:
BDBM17594
Synonyms:
A-357300 | CHEMBL352764 | N'-[(2S,3R)-3-amino-2-hydroxy-5-(propan-2-ylsulfanyl)pentanoyl]-3-chlorobenzohydrazide | bestatin-type inhibitor, 9
Type:
Small organic molecule
Emp. Form.:
C15H22ClN3O3S
Mol. Mass.:
359.871
SMILES:
CC(C)SCC[C@@H](N)[C@H](O)C(=O)NNC(=O)c1cccc(Cl)c1 |r|
Substrate
Name:
Octapeptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
819.07
Organism:
n/a
Description:
n/a
Residue:
8
Sequence:
MGKVKVGV