Reaction Details Report a problem with these data
Target
Serine protease hepsin
Ligand
BDBM50580331
Substrate
n/a
Meas. Tech.
ChEMBL_2148121 (CHEMBL5032467)
IC50
1.7±n/a nM
Citation
Damalanka, VC; Voss, JJLP; Mahoney, MW; Primeau, T; Li, S; Klampfer, L; Janetka, JW Macrocyclic Inhibitors of HGF-Activating Serine Proteases Overcome Resistance to Receptor Tyrosine Kinase Inhibitors and Block Lung Cancer Progression. J Med Chem 64:18158-18174 (2021) [PubMed] Article
More Info.:
Target
Name:
Serine protease hepsin
Synonyms:
HEPS_HUMAN | HPN | Hepsin | Serine protease hepsin | TMPRSS1 | Transmembrane protease serine 11E | Transmembrane protease, serine 1
Type:
Enzyme
Mol. Mass.:
45016.98
Organism:
Human
Description:
Human deglycosylated hepsin was expressed in Pichia pastoris.
Residue:
417
Sequence:
MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSADARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCVDEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSLRYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYHGGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQYYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCEDSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL