Reaction Details |
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Target | Urokinase-type plasminogen activator |
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Ligand | BDBM50312653 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_617823 (CHEMBL1100529) |
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Ki | >26000±n/a nM |
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Citation | Lu, T; Markotan, T; Ballentine, SK; Giardino, EC; Spurlino, J; Crysler, CS; Brown, K; Maryanoff, BE; Tomczuk, BE; Damiano, BP; Shukla, U; End, D; Andrade-Gordon, P; Bone, RF; Player, MR Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif. J Med Chem53:1843-56 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Urokinase-type plasminogen activator |
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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: | MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQ
HCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHN
YCRNPDNRRRPWCYVQVGLKPLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKII
GGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLG
RSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICL
PSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKML
CAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIR
SHTKEENGLAL
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BDBM50312653 |
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n/a |
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Name | BDBM50312653 |
Synonyms: | 1-{N-[2-(Amidinoaminooxy)ethyl]amino}carbonylmethyl-6-chloro-3-[2,2-difluoro-2-phenylethylamino]pyrazinone | CHEMBL1088332 |
Type | Small organic molecule |
Emp. Form. | C17H20ClF2N7O3 |
Mol. Mass. | 443.836 |
SMILES | [#7]\[#6](-[#7])=[#7]\[#8]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-n1c(Cl)cnc(-[#7]-[#6]C(F)(F)c2ccccc2)c1=O |
Structure |
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