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Target
Urokinase-type plasminogen activator
Ligand
BDBM23893
Substrate
BDBM23922
Meas. Tech.
Determination of Inhibition Constants
Ki
1200±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:
BDBM23893
Synonyms:
3-amidinophenylalanine deriv., 37 | N-(2-aminoethyl)-1-[(2S)-3-(3-carbamimidoylphenyl)-2-{[2,4,6-tris(propan-2-yl)benzene]sulfonamido}propanoyl]piperidine-4-carboxamide
Type:
Small organic molecule
Emp. Form.:
C33H50N6O4S
Mol. Mass.:
626.853
SMILES:
CC(C)c1cc(C(C)C)c(c(c1)C(C)C)S(=O)(=O)N[C@@H](Cc1cccc(c1)C(N)=N)C(=O)N1CCC(CC1)C(=O)NCCN |r|