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Target
Urokinase-type plasminogen activator
Ligand
BDBM16131
Substrate
BDBM14716
Meas. Tech.
Determination of Inhibitor Potency and Selectivity
pH
8.1±n/a
Temperature
310.15±n/a K
Ki
160±n/a nM
Km
90000±n/a nM
Citation
Fish, PV; Barber, CG; Brown, DG; Butt, R; Collis, MG; Dickinson, RP; Henry, BT; Horne, VA; Huggins, JP; King, E; O'gara, M; McCleverty, D; McIntosh, F; Phillips, C; Webster, R Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines. J Med Chem 50:2341-51 (2007) [PubMed] Article
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:
BDBM16131
Synonyms:
1-guanidino-7-sulfonamidoisoquinoline 5 | 2-[7-(phenylsulfamoyl)isoquinolin-1-yl]guanidine
Type:
Small organic molecule
Emp. Form.:
C16H15N5O2S
Mol. Mass.:
341.388
SMILES:
[#7]\[#6](-[#7])=[#7]/c1nccc2ccc(cc12)S(=O)(=O)[#7]-c1ccccc1
Substrate
Name:
BDBM14716
Synonyms:
(2S)-5-carbamimidamido-N-(4-nitrophenyl)-2-(2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}acetamido)pentanamide hydrochloride | Chromogenic Substrate S-2444 | L-Pyroglutamyl-glycyl-L-argininep-Nitroaniline hydrochloride
Type:
Small organic molecule
Emp. Form.:
C19H26N8O6
Mol. Mass.:
462.4597
SMILES:
[#7]\[#6](-[#7])=[#7]/[#6]-[#6]-[#6]-[#6@H](-[#7]-[#6](=O)-[#6]-[#7]-[#6](=O)-[#6@@H]-1-[#6]-[#6]-[#6](=O)-[#7]-1)-[#6](=O)-[#7]-c1ccc(cc1)-[#7+](-[#8-])=O |r|