Target
Methionine aminopeptidase 2
Ligand
BDBM17480
Substrate
Octapeptide substrate
Meas. Tech.
MetAP2 Enzyme Activity Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
31±n/a nM
Citation
 Sheppard, GSWang, JKawai, MFidanze, SDBaMaung, NYErickson, SABarnes, DMTedrow, JSKolaczkowski, LVasudevan, APark, DCWang, GTSanders, WJMantei, RAPalazzo, FTucker-Garcia, LLou, PZhang, QPark, CHKim, KHPetros, AOlejniczak, ENettesheim, DHajduk, PHenkin, JLesniewski, RDavidsen, SKBell, RL Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding. J Med Chem 49:3832-49 (2006) [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:
BDBM17480
Synonyms:
2-[(2-{[2-(diethylamino)ethyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid | Anthranilic Acid Sulfonamide, 10b
Type:
Small organic molecule
Emp. Form.:
C23H31N3O4S
Mol. Mass.:
445.575
SMILES:
CCN(CC)CCNc1ccccc1S(=O)(=O)Nc1ccc2CCCCc2c1C(O)=O
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