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Target
Urokinase-type plasminogen activator [179-431,I214M,N322A,S371A]
Ligand
BDBM14169
Substrate
BDBM14484
Meas. Tech.
Enzyme Assay and Determination of the Inhibition Constants
Ki
1700±n/a nM
Citation
 Katz, BA; Luong, C; Ho, JD; Somoza, JR; Gjerstad, E; Tang, J; Williams, SR; Verner, E; Mackman, RL; Young, WB; Sprengeler, PA; Chan, H; Mortara, K; Janc, JW; McGrath, ME Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA). J Mol Biol 344:527-47 (2004) [PubMed]  Article 
Target
Name:
Urokinase-type plasminogen activator [179-431,I214M,N322A,S371A]
Synonyms:
LMW uPA | PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase (uPA) Mutant (S190A) | deglycosylated (N145A) LMW uPA Mutant S190A
Type:
Enzyme
Mol. Mass.:
28389.65
Organism:
Homo sapiens (Human)
Description:
Mutagenically deglycosylated (N145A) low molecular mass urokinase (S190A), referred to as Ala190 uPA.
Residue:
253
Sequence:
IIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLMSPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKEASTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDACQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
  
Inhibitor
Name:
BDBM14169
Synonyms:
4-Iodobenzo[b]thiophene-2-carboxamidine | APC-6860 | CA-01 | CRA-6860 | [amino(4-iodo-1-benzothiophen-2-yl)methylidene]azanium
Type:
Small organic molecule
Emp. Form.:
C9H8IN2S
Mol. Mass.:
303.142
SMILES:
NC(=[NH2+])c1cc2c(I)cccc2s1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM14484
Synonyms:
4-{[({4-carbamimidamido-1-[(4-methyl-2-oxo-2H-chromen-7-yl)carbamoyl]butyl}carbamoyl)methyl]carbamoyl}butanoic acid hydrochloride | Glutaryl-Gly-Arg-7-amido-4-methylcoumarin | uPA Substrate
Type:
n/a
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: