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Target
Urokinase-type plasminogen activator
Ligand
BDBM14350
Substrate
BDBM14484
Meas. Tech.
Enzyme Assay and Determination of the Inhibition Constants
Ki
30±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:
3.4.21.73 | PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator chain B | Urokinase-type plasminogen activator long chain A | Urokinase-type plasminogen activator short chain A | Urokinase-type plasminogen activator/surface receptor | uPA
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Homo sapiens (Human)
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKLLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
Inhibitor
Name:
BDBM14350
Synonyms:
2-{5-[amino(iminiumyl)methyl]-6-fluoro-1H-1,3-benzodiazol-2-yl}-6-{[(1S,2S)-2-methylcyclohexyl]oxy}benzen-1-olate | CA-11 | CRA-11092
Type:
Small organic molecule
Emp. Form.:
C21H23FN4O2
Mol. Mass.:
382.4313
SMILES:
C[C@H]1CCCC[C@@H]1Oc1cccc(-c2nc3cc(C(N)=[NH2+])c(F)cc3[nH]2)c1[O-] |r|