Reaction Details |
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Target | Urokinase-type plasminogen activator |
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Ligand | BDBM14149 |
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Substrate/Competitor | BDBM13949 |
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Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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Ki | 11±n/a nM |
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Citation | Katz, BA; Sprengeler, PA; Luong, C; Verner, E; Elrod, K; Kirtley, M; Janc, J; Spencer, JR; Breitenbucher, JG; Hui, H; McGee, D; Allen, D; Martelli, A; Mackman, RL Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets. Chem Biol8:1107-21 (2001) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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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BDBM14149 |
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BDBM13949 |
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Name | BDBM14149 |
Synonyms: | 6-fluoro-2-(2-hydroxy-3-{[(1S,2S)-2-methylcyclohexyl]oxy}phenyl)-1H-indole-5-carboximidamide | APC-11092 |
Type | Small organic molecule |
Emp. Form. | C22H24FN3O2 |
Mol. Mass. | 381.4433 |
SMILES | C[C@H]1CCCC[C@@H]1Oc1cccc(-c2cc3cc(C(N)=N)c(F)cc3[nH]2)c1O |r| |
Structure |
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