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Target
Transmembrane protease serine 2
Ligand
BDBM525256
Substrate
n/a
Meas. Tech.
TMPRSS2 pericellular activity screening assay
IC50
5.20±5.40 nM
Citation
 Shapira, T; Monreal, IA; Dion, SP; Buchholz, DW; Imbiakha, B; Olmstead, AD; Jager, M; Désilets, A; Gao, G; Martins, M; Vandal, T; Thompson, CAH; Chin, A; Rees, WD; Steiner, T; Nabi, IR; Marsault, E; Sahler, J; Diel, DG; Van de Walle, GR; August, A; Whittaker, GR; Boudreault, PL; Leduc, R; Aguilar, HC; Jean, F A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic. Nature 0:0 (2022) [PubMed]  Article 
Target
Name:
Transmembrane protease serine 2
Synonyms:
Transmembrane protease serine 2 catalytic chain | Serine protease 10 | Transmembrane protease serine 2 non-catalytic chain | TMPS2_HUMAN | TMPRSS2 | PRSS10
Type:
PROTEIN
Mol. Mass.:
53867.70
Organism:
Human
Description:
ChEMBL_760112
Residue:
492
Sequence:
MALNSGSPPAIGPYYENHGYQPENPYPAQPTVVPTVYEVHPAQYYPSPVPQYAPRVLTQASNPVVCTQPKSPSGTVCTSKTKKALCITLTLGTFLVGAALAAGLLWKFMGSKCSNSGIECDSSGTCINPSNWCDGVSHCPGGEDENRCVRLYGPNFILQVYSSQRKSWHPVCQDDWNENYGRAACRDMGYKNNFYSSQGIVDDSGSTSFMKLNTSAGNVDIYKKLYHSDACSSKAVVSLRCIACGVNLNSSRQSRIVGGESALPGAWPWQVSLHVQNVHVCGGSIITPEWIVTAAHCVEKPLNNPWHWTAFAGILRQSFMFYGAGYQVEKVISHPNYDSKTKNNDIALMKLQKPLTFNDLVKPVCLPNPGMMLQPEQLCWISGWGATEEKGKTSEVLNAAKVLLIETQRCNSRYVYDNLITPAMICAGFLQGNVDSCQGDSGGPLVTSKNNIWWLIGDTSWGSGCAKAYRPGVYGNVMVFTDWIYRQMRADG
  
Inhibitor
Name:
BDBM525256
Synonyms:
N-0438 | (H)Arg-Glu-Phe-Arg-kbt
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)c1nc2ccccc2s1 |r|
Structure:
Search PDB for entries with ligand similarity: