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Details of RareLED ID Assay_1014
Primary information
GENECTSK
NUMBER OF ASSAY179
ASSAY IDs255862 255213 51175 48400 261373 257083 48397 219369 219368 219367 219366 51180 48411 48410 48409 48405 48404 48399 48398 1241503 273237 51185 51179 746595 266476 262994 240844 240722 51184 339652 314228 314219 259958 51200 51193 51174 48406 1258333 339477 328995 310230 308310 288395 277532 254915 254886 254881 242090 241950 240845 240716 240649 239258 238235 51181 48414 51177 48413 48412 48403 219371 51204 48418 677816 466811 358949 268736 254421 51178 747794 722934 722933 703431 691904 691899 609673 609670 554256 448876 448879 699423 367816 365199 364997 307274 307165 293182 264113 263488 262143 260670 242466 242310 48407 51202 51201 51197 51176 48408 526076 493662 466514 468523 351473 51173 1299800 259959 1259028 1258317 1257953 370550 367439 361731 358950 321237 308316 271488 270167 262402 242447 51186 51205 570623 569575 493850 1322988 722939 722935 70343
Assay Name1. In vitro inhibitory concentration against cathepsin K in cell-based assay of bone resorption,2. Apparent inhibitory constant against human cathepsin K,3. In vitro inhibitory activity against Human Cathepsin K using 2 uM of Z -Leu-Arg-AMC as substrate,4. In vitro inhibitory activity against human cathepsin K, using 2 uM of Z -Leu-Arg-AMC as substrate,5. Inhibition of human cathepsin K,6. Inhibitory activity against humanized rabbit cathepsin K,7. Concentration required to inhibit 50% of cysteine protease cathepsin K of human,8. Inhibition of Human cathepsin K,9. in vitro cell based assay for measuring the IC50 values of osteoblast resorption.,10. In vitro cell based assay for measuring the IC50 values of osteoblast resorption.,11. In vitro IC50 value was measured using in situ cytochem assay.,12. Inhibitory constant against human cathepsin K,13. Inhibitory activity tested against Human Cathepsin K using Z-Phe-Arg-pNA as substrate,14. Inhibitory activity tested against Human Cathepsin K receptor using gelatinase assay,15. Inhibitory activity tested against Human Cathepsin K receptor using bone resorption assay,16. Inhibition of Cathepsin K at pH 7,17. Inhibition of Cathepsin K at pH 5.5,18. Effect of 10 mM of GSH on the inhibitory activity against Cathepsin K, at pH 7,19. Effect of 10 mM of GSH on the inhibitory activity of compound against Cathepsin K, at pH 5.5,20. Inhibition of human cathepsin-K using Z-Gly-Pro-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay,21. Inhibition of cathepsin K,22. In vitro inhibition of human Cathepsin K.,23. Inhibitory activity tested against human Cathepsin K,24. Inhibition of recombinant cathepsin-K (unknown origin) using Z-Phe-Arg-AMC as substrate by fluorescence assay,25. Inhibition of human cathepsin K,26. Inhibition of humanized rabbit Cathepsin K,27. Inhibitory potency against human Cathepsin K,28. Inhibitory concentration against human cathepsin K,29. Inhibitory activity measured against cathepsin K.,30. Inhibition of human recombinant cathepsin K by fluorescence assay,31. Inhibition of human cathepsin K,32. Inhibition of humanized rabbit cathepsin K,33. Inhibitory activity against humanized rabbit Cathepsin K,34. Eq. constant (Ki) for inhibition of Cathepsin K was determined by progress curves, following hydrolysis of Z-Phe-Arg- Amc in the absence and presence of compound,35. Inhibition of recombinant rabbit Cathepsin K in a fluorescence assay,36. Inhibition of Human Cathepsin K,37. Inhibition of recombinant human cathepsin K in fluorescence assay,38. Biological Assay: Recombinant human procathepsin K was obtained from Enzo Life Sciences. Activation of the proenzyme was performed in 32.5 mM sodium acetate pH 3.5, EDTA 1 mM, NaCl 500 mM, human procathepsin K 5.5 uM, at room temperature. Activation times were optimized and varied between 35 and 150 minutes. Cathepsin K was preincubated with test compounds at various concentrations for 5 minutes at 25C. The assay was initiated by addition of substrate Z-Phe-Arg-aminomethylcoumarin ("Z-F-R-AMC" Bacchem) and the final assay conditions were 1.5 nM cathepsin K, 50 uM Z-F-R-AMC, 150 mM sodium acetate pH 5.5, 2.5 mM EDTA (Omnipure), 2.5 mM DTT (EMD), 0.01% BRIJ 35 (Sigma), and 4.0% DMSO (Acros). Test compounds were serially diluted with DMSO and water to include a final concentration range of 10 uM to 10 pM. The reaction was monitored fluorometrically for 5 minutes at 25C. using black 96-well Corning 3686 assay microplates with a Thermo Fluoroskan Ascent FL microplate reader.,39. Inhibition of human recombinant cathepsin K,40. Inhibition of human recombinant cathepsin K by fluorescence assay,41. Inhibition of cathepsin K by fluorescence assay,42. Inhibition of humanized rabbit cathepsin K,43. Inhibition of cathepsin K,44. Inhibition of human recombinant cathepsin K,45. Inhibitory activity against cathepsin K (10 pM) using humanized rabbit enzyme,46. Inhibitory activity against cathepsin K using humanized rabbit enzyme,47. Inhibitory activity against cathepsin K from humanized rabbit enzyme,48. Inhibition of 10 uM Cbz-Phe-Arg-AMC binding to human cathepsin K in fluorescence assay,49. Inhibitory concentration against human cathepsin K using 10 uM Cbz-Phe-Arg-AMC,50. Inhibitory potency against human Cathepsin K,51. Inhibitory concentration against human cathepsin K,52. Inhibition of human cathepsin K,53. Inhibition constant against human cathepsin K in fluorescence assay using Cbz-Phe-Arg-AMC,54. Inhibition constant against human cathepsin K,55. Specificity of Cathepsin K inhibition by the compound,56. Inhibitory constant against human cathepsin K,57. Inhibitory activity against recombinant human cathepsin K,58. Inhibitory concentration against recombinant human cathepsin K determined in a fluorescence assay using 10 uM Cbz-Phe-Arg-AMC as substrate,59. Inhibitory concentration against recombinant human cathepsin K,60. Inhibitory activity against recombinant human cathepsin K,61. Inhibitory activity was evaluated against cathepsin K,62. Inhibition of cathepsin K,63. Binding affinity against cathepsin K,64. Inhibition of human recombinant cathepsin K using Z-Phe-Arg-AMC as substrate preincubated for 30 mins measured after 1 hr by quenched fluorescent resonance energy transfer assay,65. Inhibition of human recombinant cathepsin K by fluorescence assay,66. Inhibition of cathepsin K by fluorimetric assay,67. Inhibition of human cathepsin K,68. Inhibitory concentration against recombinant human Cathepsin K at 37 degree C at pH 5.5,69. Inhibitory activity was measured against Cathepsin K,70. Inhibition of human cathepsin-K,71. Inhibition of human cathepsin K by gelatin zymographic analysis,72. Inhibition of human cathepsin K,73. Inhibition of human recombinant cathepsin-k using Z-Phe-Arg-AMC as substrate preincubated for 15 mins measured after 1 hr by QFRET assay,74. Inhibition of human cathepsin K using Z-Leu-Arg-AMC as substrate after 80 mins by fluorimetric analysis,75. Inhibition of human cathepsin K using Z-Leu-Arg-AMC as substrate after 10 mins by fluorimetric analysis,76. Inhibition of human recombinant cathepsin K using z-LR-AFC as substrate by fluorescence assay,77. Inhibition of human cathepsin K using Z-Lys-Gln-Lys-Leu-Arg-AMC as substrate after 1 hr by fluorescence assay,78. Inhibition of human recombinant cathepsin K after 30 mins by spectrophotometric assay,79. Inhibition of cathepsin K after 10 to 15 mins by fluorescence assay,80. Inhibition of cathepsin X after 10 to 15 mins by fluorescence assay,81. Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage incubated for 1 hrs by QFRET assay,82. Inhibition of human recombinant cathepsin K expressed in baculovirus by fluorescence assay,83. Inhibition of human recombinant cathepsin K by fluorescence assay,84. Inhibition of human recombinant cathepsin K by fluorescence assay,85. Inhibition of humaized rabbit cathepsin K,86. Inhibition of cathepsin K,87. Inhibition of human recombinant cathepsin K,88. Inhibition of recombinant human cathepsin K,89. Inhibition of Cathepsin K,90. Inhibitory activity against recombinant human Cathepsin K,91. Inhibition of recombinant human cathepsin K in a fluorescence assay,92. Inhibition of 10 lM Cbz-Phe-Arg-AMC binding to human cathepsin K in fluorescence assay with 100 mM NaOAc,93. Inhibitory concentration against recombinant human cathepsin K by using Z-Phe-Arg-AMC as synthetic substrate,94. Inhibitory activity against human cathepsin K,95. Inhibitory activity against cathepsin K,96. Inhibitory activity against Cathepsin K,97. Inhibitory activity against Cathepsin K,98. Inhibitory activity against human cysteine protease, cathepsin K.,99. Inhibitory activity against recombinant human cathepsin K activity using fluorescence assay,100. Inhibition of human recombinant cathepsin K using Z-Phe-Arg-MCA substrate by fluorimetric assay,101. Inhibition of human recombinant cathepsin K,102. Inhibition of human recombinant cathepsin K by fluorescence assay,103. Inhibition of human cathepsin K,104. Inhibition of cathepsin K,105. Compound was tested for its inhibitory activity against human osteoclast cathepsin K,106. Inhibition of human recombinant cathepsin K using Cbz-Leu-Arg-AMC as substrate incubated for 30 mins measured for 20 mins by spectrofluorometrical analysis,107. Inhibitory activity against human Cathepsin K,108. Inhibition Assay: To activate the proenzyme, 5 ul procathepsin K were mixed with 1 ul activation buffer, and incubated at room temperature for 30 min.5 uL test compound (final concentration 0.1 nM to 100 uM) in aqua bidest (containing 4% DMSO, final DMSO concentration 1%) were mixed with 10 uL of Cathepsin K in assay buffer (final concentration 2 ng/uL) and incubated for 10 min. Then 5 uL of substrate in assay buffer (final concentration 12.5 uM) were added. The plates were then incubated at room temperature for 60 min. Then, the reaction was stopped by adding 10 uL of E64 in assay buffer (final concentration 1 uM). The fluorescence in the wells was determined using a Molecular Devices SpectraMax M5 Fluorescence Reader (Ex 360 nm, Em 460 nm).Each assay microtiter plate contains wells with vehicle controls (1% DMSO in bidest) as reference for non-inhibited enzyme activity (100% Ctl; high values) and wells with inhibitor (E64 in bidest+1% DMSO.,109. Inhibition Assay: The following buffers were used: Activation buffer: 32.5 mM sodium acetate, adjusted to pH 3.5 with HCl; Assay buffer: 150 mM sodium acetate, 4mM EDTA, 20 mM L-Cysteine, adjusted to pH 5.5 with HCl,Assay conditions: To activate the proenzyme, 5 uLprocathepsin K were mixed with 1 ul activation buffer, and incubated at room temperature for 30 min. 5 uL test compound (final concentration 0.1 nM to 100 uM) in aqua bidest (containing 4% DMSO, final DMSO concentration 1%) were mixed with 10 uL of Cathepsin K in assay buffer (final concentration 2 ng/uL) and incubated for 10 min. Then 5 uL
ACTIVITYSubstance BioActivity: 1 Active, 1 Activity <= 1 µM, 1 Tested Substance BioActivity: 8 Active, 3 Activity <= 1 nM, 8 Activity <= 1 µM, 9 Tested Substance BioActivity: 1 Active, 1 Activity <= 1 µM, 1 Tested Substance BioActivity: 40 Active, 34 Activity <= 1 µM, 41 Tested Substance BioActivity: 13 Active, 4 Activity <= 1 nM, 13 Activity <= 1 µM, 13 Tested Substance BioActivity: 6 Active, 1 Activity <= 1 nM, 5 Activity <= 1 µM, 6 Tested Substance BioActivity: 40 Active, 9 Activity <= 1 nM, 39 Activity <= 1 µM, 40 Tested Substance BioActivity: 14 Active, 2 Activity <= 1 nM, 15 Activity <= 1 µM, 15 Tested Substance BioActivity: 1 Active, 1 Activity <= 1 µM, 1 Tested Substance BioActivity: 1 Active, 1 Activity <= 1 µM, 1 Tested Substance BioActivity: 2 Active, 2 Activity <= 1 µM, 2 Tested Substance BioActivity: 4 Active, 4 Activity <= 1 µM, 4 Tested Substance BioActivity: 16 Active, 14 Activity <= 1 µM, 17 Tested Substance BioActivity: 4 Active, 4 Activity <= 1 µM, 4 Tested Sub