Reaction Details Report a problem with these data
Target
Urokinase-type plasminogen activator
Ligand
BDBM23911
Substrate
BDBM23922
Meas. Tech.
Determination of Inhibition Constants
Ki
3400±n/a nM
Citation
Steinmetzer, T; Schweinitz, A; Stürzebecher, A; Dönnecke, D; Uhland, K; Schuster, O; Steinmetzer, P; Müller, F; Friedrich, R; Than, ME; Bode, W; Stürzebecher, J Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. J Med Chem 49:4116-26 (2006) [PubMed] Article
More Info.:
Target
Name:
Urokinase-type plasminogen activator
Synonyms:
PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator/surface receptor
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Homo sapiens (Human)
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKPLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
Inhibitor
Name:
BDBM23911
Synonyms:
3-[(2S)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-3-oxo-2-[(6-phenoxypyridine-3-)sulfonamido]propyl]benzene-1-carboximidamide | 3-amidinophenylalanine deriv., 54
Type:
Small organic molecule
Emp. Form.:
C29H36N8O4S
Mol. Mass.:
592.712
SMILES:
[#7]\[#6](-[#7])=[#7]\[#6]-[#6]-[#6]-1-[#6]-[#6]-[#7](-[#6]-[#6]-1)-[#6](=O)-[#6@H](-[#6]-c1cccc(c1)-[#6](-[#7])=[#7])-[#7]S(=O)(=O)c1ccc(-[#8]-c2ccccc2)nc1 |r|