Reaction Details Report a problem with these data
Target
Methionine aminopeptidase 2
Ligand
BDBM17617
Substrate
Octapeptide substrate
Meas. Tech.
MetAP2 Enzyme Activity Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
8±n/a nM
Citation
 Wang, GT; Mantei, RA; Kawai, M; Tedrow, JS; Barnes, DM; Wang, J; Zhang, Q; Lou, P; Garcia, LA; Bouska, J; Yates, M; Park, C; Judge, RA; Lesniewski, R; Sheppard, GS; Bell, RL Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids. Bioorg Med Chem Lett 17:2817-22 (2007) [PubMed]  Article 
Target
Name:
Methionine aminopeptidase 2
Synonyms:
Initiation factor 2-associated 67 kDa glycoprotein | MAP 2 | MAP2_HUMAN | METAP2 | MNPEP | MetAP 2 | Methionine aminopeptidase 2 (MetAP2) | Methionine aminopeptidases (HsMetAP2) | P67EIF2 | Peptidase M 2 | p67
Type:
Enzyme
Mol. Mass.:
52884.45
Organism:
Homo sapiens (Human)
Description:
P50579
Residue:
478
Sequence:
MAGVEEVAASGSHLNGDLDPDDREEGAASTAEEAAKKKRRKKKKSKGPSAAGEQEPDKESGASVDEVARQLERSALEDKERDEDDEDGDGDGDGATGKKKKKKKKKRGPKVQTDPPSVPICDLYPNGVFPKGQECEYPPTQDGRTAAWRTTSEEKKALDQASEEIWNDFREAAEAHRQVRKYVMSWIKPGMTMIEICEKLEDCSRKLIKENGLNAGLAFPTGCSLNNCAAHYTPNAGDTTVLQYDDICKIDFGTHISGRIIDCAFTVTFNPKYDTLLKAVKDATNTGIKCAGIDVRLCDVGEAIQEVMESYEVEIDGKTYQVKPIRNLNGHSIGQYRIHAGKTVPIVKGGEATRMEEGEVYAIETFGSTGKGVVHDDMECSHYMKNFDVGHVPIRLPRTKHLLNVINENFGTLAFCRRWLDRLGESKYLMALKNLCDLGIVDPYPPLCDIKGSYTAQFEHTILLRPTCKEVVSRGDDY
  
Inhibitor
Name:
BDBM17617
Synonyms:
5,6-disubstituted anthranilic acid sulfonamide, 9i | 6-[(4-fluorobenzene)sulfonamido]-3-(furan-3-yl)-2-methoxybenzoic acid
Type:
Small organic molecule
Emp. Form.:
C18H14FNO6S
Mol. Mass.:
391.37
SMILES:
COc1c(ccc(NS(=O)(=O)c2ccc(F)cc2)c1C(O)=O)-c1ccoc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Octapeptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
819.07
Organism:
n/a
Description:
n/a
Residue:
8
Sequence:
MGKVKVGV