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Target
Methionine aminopeptidase 2
Ligand
BDBM468959
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay of MetAP2
IC50
155±27 nM
Citation
 Ho, KK; Quan, W; Zhou, J Pyrrolidinone compounds US Patent  US10807971 Publication Date 10/20/2020 
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:
BDBM468959
Synonyms:
1-[2-[4-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tetrahydropyran-3-yl]piperazin-1-yl]pyrimidin-5-yl]-N-[(2,3-difluorophenyl)methyl]-3-hydroxy-2-oxo-pyrrolidine-3-carboxamide, isomer 1 hydrochloride | US10807971, Example 3
Type:
Small organic molecule
Emp. Form.:
C31H33F4N7O4
Mol. Mass.:
643.6318
SMILES:
N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O |r|
Structure:
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