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Details of RareLED ID Assay_1010

Primary information
GENE	CTSC
NUMBER OF ASSAY	37
ASSAY IDs	370555 370553 370552 365004 360102 314225 290153 268072 56058 56057 56056 1259027 1258745 1258680 1258376 1258316 1258310 1177065 1138553 1138552 47821 612807 570622 503871 470223 448872 444704 1320494 1320493 1320492 1320491 1320489 1320476 1320475 1320474 1320454 1320453
Assay Name	1. Inhibition of human recombinant cathepsin C by fluorescence assay,2. Inhibition of cathepsin C in human B721 cells by FACS assay,3. Blockade of conjugation of cathepsin C in human B721 cells to I125-labeled (S)-2-amino-N-((S)-1-(4-hydroxy-3-iodophenylsulfonyl)-5-phenylpent-1-en-3-yl)pentanamide pretreated for 30 mins before addition of I125-labeled (S)-2-amino-N-((S)-1-(4-hydroxy-3-iodophenylsulfonyl)-5-phenylpent-1-en-3-yl)pentanamide by SDS-PAGE,4. Inhibition of human cathepsin C,5. Inhibition of human recombinant cathepsin C after 10 mins,6. Inhibition of cathepsin C,7. Inhibition of human recombinant cathepsin C,8. Inhibition of human DPP1,9. Michaelis constant against Dipeptidyl aminopeptidase 1,10. Compound was tested for Inhibition of dipeptidyl Dipeptidyl aminopeptidase 1,11. Compound was tested for Inhibition of Dipeptidyl aminopeptidase 1,12. Inhibition Assay: The recombinant human DPPI was diluted in TAGZyme buffer to 1 U/ml (38.1 ug/ml, respectively), and then activated by mixing in a 1:2 ratio with a Cysteamine aqueous solution (2 mM) and incubating for 5 min at room temperature.Five 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 DPPI in MES buffer (final concentration 0.0125 ng/uL) and incubated for 10 min. Then, 5 uL of substrate in MES buffer (final concentration 50 uM) were added. The microtiter plates were then incubated at room temperature for 30 min. Then, the reaction was stopped by adding 10 uL of Gly-Phe-DMK in MES-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) or an Envision Fluorescence Reader (Ex 355 nm, Em 460 nm).,13. Inhibition Assay: The following buffers were used: MES buffer: 25 mM MES, 50 mM NaCl, 5 mM DTT, adjusted to pH 6.0, containing 0.1% BSA; TAGZyme Buffer: 20 mM NaH2PO4, 150 mM NaCl adjusted to pH 6.0 with HCl. Assay Conditions: The recombinant human DPPI was diluted in TAGZyme buffer to 1 U/ml (38.1 ug/ml, respectively), and then activated by mixing in a 1:2 ratio with a Cysteamine aqueous solution (2 mM) and incubating for 5 min at room temperature.Five 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 DPPI in MES buffer (final concentration 0.0125 ng/uL) and incubated for 10 min. Then, 5 uL of substrate in MES buffer (final concentration 50 uM) were added. The microtiter plates were then incubated at room temperature for 30 min. Then, the reaction was stopped by adding 10 uL of Gly-Phe-DMK in MES-buffer (final concentration 1 uM).,14. Inhibition Assay: The recombinant human DPPI was diluted in TAGZyme buffer to 1 U/ml (38.1 ug/ml, respectively), and then activated by mixing in a 1:2 ratio with a Cysteamine aqueous solution (2 mM) and incubating for 5 min at room temperature.Five 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 DPPI in MES buffer (final concentration 0.0125 ng/uL) and incubated for 10 min. Then, 5 uL of substrate in MES buffer (final concentration 50 uM) were added. The microtiter plates were then incubated at room temperature for 30 min. Then, the reaction was stopped by adding 10 uL of Gly-Phe-DMK in MES-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) or an Envision Fluorescence Reader (Ex 355 nm, Em 460 nm).,15. Inhbition Assay: The recombinant human DPPI was diluted in TAGZyme buffer to 1 U/ml (38.1 ug/ml, respectively), and then activated by mixing in a 1:2 ratio with a Cysteamine aqueous solution (2 mM) and incubating for 5 min at room temperature.Five 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 DPPI in MES buffer (final concentration 0.0125 ng/uL) and incubated for 10 min. Then, 5 uL of substrate in MES buffer (final concentration 50 uM) were added. The microtiter plates were then incubated at room temperature for 30 min. Then, the reaction was stopped by adding 10 uL of Gly-Phe-DMK in MES-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) or an Envision Fluorescence Reader (Ex 355 nm, Em 460 nm).,16. Inhibition Assay: The following buffers were used: MES buffer: 25 mM MES, 50 mM NaCl, 5 mM DTT, adjusted to pH 6.0, containing 0.1% BSA; TAGZyme Buffer: 20 mM NaH2P04, 150 mM NaCl adjusted to pH 6.0 with HC1Assay conditions: The recombinant human DPPI was diluted in TAGZyme buffer to 1 U/ml (38.1 ug/ml, respectively), and then activated by mixing in a 1 :2 ratio with a Cysteamine aqueous solution ( 2mM) and incubating for 5 min at room temperature.Five 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 uM of DPPI in MES buffer (final concentration 0.0125 ng/uL) and incubated for 10 min. Then, 5 uL of substrate in MES buffer (final concentration 50 uM) were added. The microtiter plates were then incubated at room temperature for 30 min. Then, the reaction was stopped by adding 10 uL of Gly-Phe-DMK in MES-buffer (final concentration 1 uM).,17. Inhibition Assay: The following buffers were used: MES buffer: 25 mM MES, 50 mM NaCl, 5 mM DTT, adjusted to pH 6.0, containing 0.1% BSA; TAGZyme Buffer: 20 mM NaH2PO4, 150 mM NaCl adjusted to pH is 6.0 with HClAssay Conditions:The recombinant human DPPI was diluted in TAGZyme buffer to 1 U/ml (38.1 ug/ml, respectively), and then activated by mixing in a 1:2 ratio with a Cysteamine aqueous solution (2 mM) and incubating for 5 mM at room temperature.Five 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 DPPI in MES buffer (final concentration 0.0125 ng/uL) and incubated for 10 min. Then, 5 uL of substrate in MES buffer (final concentration 50 uM) were added. The microtiter plates were then incubated at room temperature for 30 mM Then, the reaction was stopped by adding 10 uL of Gly-Phe-DMK in MES-buffer (final concentration 1 uM).,18. Inhibition of human recombinant Cathepsin C using fluorogenic peptide substrate,19. Inhibition of cathepsin C in human THP1 cells assessed as inhibition of H-Gly-Phe-AFC cleavage by fluorescence assay,20. Inhibition of recombinant human cathepsin C using H-Gly-Arg-AMC as substrate preincubated for 30 mins before substrate addition measured after 60 mins by fluorescence assay,21. Compound was evaluated to inhibit cathepsin C (Dipeptidyl peptidase I) in non competitive binding assay,22. Inhibition of bovine spleen cathepsin C,23. Inhibition of human recombinant cathepsin C after 1 hr,24. Binding affinity to cathepsin C in crude rat liver homogenates using [125I]DCG-04 based competition protein labeling by SDS-PAGE method,25. Inhibition of human recombinant cathepsin C,26. Inhibition of cathepsin C after 10 to 15 mins by fluorescence assay,27. Inhibition of human Cathepsin C,28. Inhibition of DPP1 in human primary bone marrow-derived CD34+ neutrophil progenitor cells assessed as inactivation of cathepsin G using N-succinyl-Ala-Ala-Pro-Phe-pNA as substrate by colorimetric method,29. Inhibition of DPP1 in human primary bone marrow-derived CD34+ neutrophil progenitor cells assessed as inactivation of proteinase 3 using aminobenzoyl-Val-Ala-Asp-Cys-Ala-Asp-Gln-ethylenediamine 2,4-dinitrophenyl as substrate by fluorometric method,30. Inhibition of DPP1 in human primary bone marrow-derived CD34+ neutrophil progenitor cells assessed as inactivation of neutrophil elastase using methoxysuccinyl-Ala-Ala-Pro-Val-AMC as substrate by fluorometric method,31. Inhibition of DPP1 in human primary bone marrow-derived CD34+ neutrophil progenitor cells,32. Reversible inhibition of human recombinant DPP1 by surface plasmon resonance direct binding assay,33. Inhibition of dog DPP1 using Gly-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorometric assay,34. Inhibition of rat DPP1 using Gly-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorometric assay,35. Inhibition of mouse DPP1 using Gly-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorometric assay,36. Inhibition of DPP1 in human U937 cells using Gly-Phe-AFC as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay,37. Inhibition of human recombinant DPP1 using Gly-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorometric assay
ACTIVITY	Substance BioActivity: 3 Active, 1 Activity <= 1 nM, 2 Activity <= 1 µM, 3 Tested Substance BioActivity: 3 Active, 1 Activity <= 1 µM, 3 Tested Substance BioActivity: 3 Active, 1 Activity <= 1 µM, 3 Tested Substance BioActivity: 1 Active, 1 Tested Substance BioActivity: 6 Active, 1 Activity <= 1 nM, 7 Activity <= 1 µM, 12 Tested Substance BioActivity: 1 Activity <= 1 µM, 1 Tested Substance BioActivity: 6 Active, 5 Activity <= 1 µM, 10 Tested Substance BioActivity: 8 Active, 6 Activity <= 1 µM, 8 Tested Substance BioActivity: 1 Tested Substance BioActivity: 1 Tested Substance BioActivity: 1 Active, 3 Tested Substance BioActivity: 24 Active, 24 Activity <= 1 µM, 24 Tested Substance BioActivity: 138 Active, 138 Activity <= 1 µM, 138 Tested Substance BioActivity: 357 Active, 13 Activity <= 1 nM, 356 Activity <= 1 µM, 357 Tested Substance BioActivity: 30 Active, 28 Activity <= 1 µM, 30 Tested Substance BioActivity: 24 Active, 24 Activity <= 1 µM, 24 Tested Substance BioActivity: