Reaction Details Report a problem with these data
Target
Methionine aminopeptidase 2
Ligand
BDBM17630
Substrate
Octapeptide substrate
Meas. Tech.
MetAP2 Enzyme Activity Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
10±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:
BDBM17630
Synonyms:
5,6-disubstituted anthranilic acid sulfonamide, 19d | 6-[(2-{[4-(dimethylamino)butyl]amino}benzene)sulfonamido]-3-ethyl-2-methoxybenzoic acid
Type:
Small organic molecule
Emp. Form.:
C22H31N3O5S
Mol. Mass.:
449.564
SMILES:
CCc1ccc(NS(=O)(=O)c2ccccc2NCCCCN(C)C)c(C(O)=O)c1OC
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