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Target
Urokinase-type plasminogen activator
Ligand
BDBM14142
Substrate
BDBM14484
Meas. Tech.
Enzyme Assay and Determination of the Inhibition Constants
Ki
33±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
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:
BDBM14142
Synonyms:
2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-6-phenylbenzen-1-olate | 3-{5-[AMINO(IMINIO)METHYL]-1H-INDOL-2-YL}-1,1-BIPHENYL-2-OLATE) | APC-8696 | CA-04 | CRA-8696
Type:
Small organic molecule
Emp. Form.:
C21H17N3O
Mol. Mass.:
327.3792
SMILES:
NC(=[NH2+])c1ccc2[nH]c(cc2c1)-c1cccc(-c2ccccc2)c1[O-]