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Target
Transmembrane protease serine 2
Ligand
BDBM525259
Substrate
n/a
Meas. Tech.
TMPRSS2 pericellular activity screening assay
IC50
>10000±n/a 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:
PRSS10 | Serine protease 10 | TMPRSS2 | TMPS2_HUMAN | Transmembrane protease serine 2 catalytic chain | Transmembrane protease serine 2 non-catalytic chain
Type:
PROTEIN
Mol. Mass.:
53867.70
Organism:
Homo sapiens (Human)
Description:
ChEMBL_760112
Residue:
492
Sequence:
MALNSGSPPAIGPYYENHGYQPENPYPAQPTVVPTVYEVHPAQYYPSPVPQYAPRVLTQASNPVVCTQPKSPSGTVCTSKTKKALCITLTLGTFLVGAALAAGLLWKFMGSKCSNSGIECDSSGTCINPSNWCDGVSHCPGGEDENRCVRLYGPNFILQVYSSQRKSWHPVCQDDWNENYGRAACRDMGYKNNFYSSQGIVDDSGSTSFMKLNTSAGNVDIYKKLYHSDACSSKAVVSLRCIACGVNLNSSRQSRIVGGESALPGAWPWQVSLHVQNVHVCGGSIITPEWIVTAAHCVEKPLNNPWHWTAFAGILRQSFMFYGAGYQVEKVISHPNYDSKTKNNDIALMKLQKPLTFNDLVKPVCLPNPGMMLQPEQLCWISGWGATEEKGKTSEVLNAAKVLLIETQRCNSRYVYDNLITPAMICAGFLQGNVDSCQGDSGGPLVTSKNNIWWLIGDTSWGSGCAKAYRPGVYGNVMVFTDWIYRQMRADG
  
Inhibitor
Name:
BDBM525259
Synonyms:
Ms-Gln-Phe-Arg-kbt(OH) | N-0385(OH)
Type:
Small organic molecule
Emp. Form.:
C28H38N8O6S2
Mol. Mass.:
646.781
SMILES:
CS(=O)(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(N)=N)C(O)c1nc2ccccc2s1 |r|
Structure:
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