| Assay ID | Title | Year | Journal | Article |
|---|
| AID1372744 | Inhibition of 20s constitutive proteasome chymotrypsin-like activity in human erythrocytes using Suc-LLVY-Glo as substrate pretreated for 2 hrs followed by substrate addition measured after 10 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Immunoproteasome inhibition and bioactivity of thiasyrbactins. |
| AID1372747 | Inhibition of immunoproteasome chymotrypsin-like activity in human erythrocytes using Suc-LLVY-Glo as substrate pretreated for 2 hrs followed by substrate addition measured after 10 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Immunoproteasome inhibition and bioactivity of thiasyrbactins. |
| AID1372748 | Inhibition of immunoproteasome caspase-like activity in human erythrocytes using Z-LRR-Glo as substrate pretreated for 2 hrs followed by substrate addition measured after 10 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Immunoproteasome inhibition and bioactivity of thiasyrbactins. |
| AID734751 | Inhibition of chymotrypsin-like activity of human constitutive 20S proteasome beta 5 subunit using biotin-(CH2)4-Leu-Leu-Leu-epoxyketone as substrate at 0.3 uM incubated for 5 mins prior to substrate addition measured after 1 hr by ELISA | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action. |
| AID1372749 | Inhibition of immunoproteasome trypsin-like activity in human erythrocytes using Z-nLPnLD-Glo as substrate pretreated for 2 hrs followed by substrate addition measured after 10 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Immunoproteasome inhibition and bioactivity of thiasyrbactins. |
| AID1372746 | Inhibition of 20s constitutive proteasome trypsin-like activity in human erythrocytes using Z-nLPnLD-Glo as substrate pretreated for 2 hrs followed by substrate addition measured after 10 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Immunoproteasome inhibition and bioactivity of thiasyrbactins. |
| AID1372745 | Inhibition of 20s constitutive proteasome caspase-like activity in human erythrocytes using Z-LRR-Glo as substrate pretreated for 2 hrs followed by substrate addition measured after 10 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Immunoproteasome inhibition and bioactivity of thiasyrbactins. |
| AID734749 | Inhibition of chymotrypsin-like activity of human 20S immunoproteasome beta 5 subunit using biotin-(CH2)4-Leu-Leu-Leu-epoxyketone as substrate at 0.3 uM incubated for 5 mins prior to substrate addition measured after 1 hr by ELISA | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action. |
| AID1779351 | Inhibition of 20s proteasome beta 5c subunit (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1612343 | Inhibition of 20S proteosome beta 1 in mouse A20 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1576780 | Inhibition of 20S proteasome beta 1c derived from human erythrocytes preincubated for 1 hr using Z-nLPnLD-Glo peptide as substrate by proteasome-glo caspase-like assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1612345 | Inhibition of 20S proteosome beta 2 in mouse A20 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1648362 | Inhibition of Beta1 subunit in human 20S proteasome using Ac-nLPnLD-AMC as substrate after 1 hr by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease. |
| AID1182712 | Inhibition of 20s proteasome subunit beta-2c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1576776 | Inhibition of human 20S proteasome beta 5i preincubated for 1 hr followed by fluorescence based assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1182707 | Inhibition of 20s proteasome subunit beta-5c in human Raji cells using BODIPY-NC005 by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1612334 | Inhibition of LMP7 in human MOLT4 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1430546 | In vivo inhibition of LMP2 in Balb/c mouse assessed as residual activity in blood at 1 mg/kg, iv administered as single bolus dose using PEG300/WFI formulation after 1 hr by ELISA relative to control | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1430542 | Stability in Balb/c mouse liver S9 fraction assessed as compound remaining at 1 uM incubated for 90 mins in absence of NADPH by LC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1612339 | Inhibition of 20S proteosome beta 2 in human MOLT4 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1182708 | Ratio of IC50 for 20s proteasome subunit beta-5c to IC50 for proteasome subunit beta-5i in human Raji cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1576791 | Inhibition of 20S proteasome beta 5i in human PBMC cells assessed as induction of PSMB6 expression at 100 nM after 3 to 72 hrs by RT-PCR analysis | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1430563 | Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1612338 | Inhibition of MECL1 in human MOLT4 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1430565 | Cytotoxicity against human PBMC assessed as decrease in cell viability by CellTiter-Glo assay | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1182714 | Ratio of IC50 for proteasome subunit beta-2i to IC50 for proteasome subunit beta-5i in human Raji cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1612341 | Inhibition of 20S proteosome beta 5 in mouse A20 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1404081 | Cytotoxicity against human NCI-H727 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1182711 | Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1430540 | Inhibition of MECL1 in human MOLT4 cell lysate after 1 hr by ELISA | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1576790 | Inhibition of 20S proteasome beta 5i in human PBMC cells assessed as induction of PSMB5 expression at 100 nM after 3 to 72 hrs by RT-PCR analysis | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1182717 | Inhibition of 20s proteasome subunit beta-5c in human RPMI8226 cells using BODIPY-NC005 by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1612390 | Inhibition of LMP7 in human PBMC at 250 nM by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1404055 | Inhibition of human 20S immunoproteasome beta-5 using Suc-LLVY-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1182709 | Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1404065 | Inhibition of human 20S immunoproteasome beta-2 at 50 uM using BocLRR-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1576778 | Selectivity ratio, ratio of IC50 for 20S proteasome beta 5c (unknown origin) to IC50 for human 20S proteasome beta 1i | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1648363 | Inhibition of LMP7 in human 20S immunoproteasome using Ac-ANW-AMC as substrate after 1 hr by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease. |
| AID1182715 | Ratio of IC50 for 20s proteasome subunit beta-2c to IC50 for proteasome subunit beta-5i in human Raji cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1576779 | Inhibition of human 20S proteasome beta 1i | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1182722 | Ratio of IC50 for 20s proteasome subunit beta-5c to IC50 for proteasome subunit beta-5i in human RPMI8226 cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1612342 | Inhibition of LMP2 in mouse A20 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1182713 | Ratio of IC50 for proteasome subunit beta-1i to IC50 for proteasome subunit beta-5i in human Raji cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1779343 | Inhibition of caspase-like activity of human proteasome beta-1c subunit using SUC-LLE-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1404061 | Inhibition of human 20S immunoproteasome beta-1 at 50 uM using Ac-PAL-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1612353 | Antiinflammatory activity in human PBMC assessed as reduction in LPS-stimulated TNF-alpha expression at 250 nM preincubated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1404079 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1404054 | Inhibition of human 20S constitutive proteasome beta-5 using Suc-LLVY-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1612335 | Inhibition of 20S proteosome beta 5 in human MOLT4 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1182710 | Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1430541 | Inhibition of proteasome beta2 in human MOLT4 cell lysate after 1 hr by ELISA | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1182716 | Inhibition of proteasome subunit beta-5i in human RPMI8226 cells using BODIPY-NC005 by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1404063 | Inhibition of human 20S immunoproteasome beta-2 using BocLRR-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1182725 | Ratio of IC50 for 20s proteasome subunit beta-2c to IC50 for proteasome subunit beta-5i in human RPMI8226 cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1612344 | Inhibition of MECL1 in mouse A20 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1779344 | Inhibition of human caspase-like activity of 20s proteasome beta 1i subunit using SUC-PAL-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1612333 | Solubility of the compound in phosphate buffer at pH 7.2 at 10 mg/ml after 24 hrs by HPLC-UV method | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1430538 | Inhibition of LMP7 in human MOLT4 cell lysate after 1 hr by ELISA | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1612355 | Antiinflammatory activity in human PBMC assessed as reduction in LPS-stimulated p40 subunit of IL-12/33 expression at 250 nM preincubated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1576777 | Selectivity ratio, ratio of IC50 for 20S proteasome beta 5c (unknown origin) to IC50 for human 20S proteasome beta 5i | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1648359 | Inhibition of LMP2 in human 20S immunoproteasome using Ac-PAL-AMC as substrate after 1 hr by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease. |
| AID1128235 | Inhibition of beta5i subunit of immunoproteasome (unknown origin) by active-site ELISA | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates. |
| AID1404057 | Inhibition of human 20S immunoproteasome beta-5 at 50 uM using Suc-LLVY-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1182724 | Ratio of IC50 for proteasome subunit beta-2i to IC50 for proteasome subunit beta-5i in human RPMI8226 cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1404060 | Inhibition of human 20S constitutive proteasome beta-1 at 50 uM using Z-LLE-betaNA as substrate incubated for 15 mins measured for 45 mins by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1430562 | Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced GMCSF production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1404062 | Inhibition of human 20S constitutive proteasome beta-2 using BocLRR-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1430547 | In vivo inhibition of LMP7 in Balb/c mouse assessed as residual activity in blood at 1 mg/kg, iv administered as single bolus dose using PEG300/WFI formulation after 1 hr by ELISA relative to control | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1576792 | Inhibition of 20S proteasome beta 5i in human PBMC cells assessed as induction of PSMB7 expression at 100 nM after 3 to 72 hrs by RT-PCR method | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1430543 | Stability in Sprague-Dawley rat liver S9 fraction assessed as compound remaining at 1 uM incubated for 90 mins in absence of NADPH by LC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1612391 | Inhibition of LMP2 in human PBMC at 250 nM by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1430544 | Stability in human liver S9 fraction assessed as compound remaining at 1 uM incubated for 90 mins in absence of NADPH by LC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1779341 | Inhibition of human proteasome subunit beta-5i chymotrypsin like activity using SUC-ANW-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1404077 | Cytotoxicity against human Caco2 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1404076 | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1612392 | Inhibition of MECL1 in human PBMC at 250 nM by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1182706 | Inhibition of proteasome subunit beta-5i in human Raji cells using BODIPY-NC005 by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1430559 | Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-12/23 p40 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1404056 | Inhibition of human 20S constitutive proteasome beta-5 at 50 uM using Suc-LLVY-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1182719 | Inhibition of 20s proteasome subunit beta-1c in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1404078 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1779345 | Inhibition of human trypsin-like activity of 20s proteasome beta 2c subunit using SUC-KQL-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1779342 | Inhibition of chymotrypsin-like activity of human 20s proteasome beta 5c subunit using suc-WLA-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1430539 | Inhibition of proteasome beta5 in human MOLT4 cell lysate after 1 hr by ELISA | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1779349 | Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1430537 | Inhibition of proteasome beta1 in human MOLT4 cell lysate after 1 hr by ELISA | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1612356 | Antiinflammatory activity in human PBMC assessed as reduction in anti-CD3/CD28 antibody-stimulated TNF-alpha expression at 250 nM preincubated for 1 hr followed by anti-CD3/CD28 antibody stimulation measured after 24 hrs by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1612340 | Inhibition of LMP7 in mouse A20 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1576775 | Inhibition of 20S proteasome beta 5c (unknown origin) preincubated for 1 hr followed by fluorescence based assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability. |
| AID1430548 | In vivo inhibition of proteasome beta5 in Balb/c mouse assessed as residual activity in blood at 1 mg/kg, iv administered as single bolus dose using PEG300/WFI formulation after 1 hr by ELISA relative to control | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1404064 | Inhibition of human 20S constitutive proteasome beta-2 at 50 uM using BocLRR-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1733118 | Inhibition of 20S immunoproteasome beta 5 chymotrypsin-like activity in human H226 cell using Suc-LLVY-AMC as substrate for 10 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities. |
| AID1612337 | Inhibition of 20S proteosome beta 1 in human MOLT4 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1182723 | Ratio of IC50 for proteasome subunit beta-1i to IC50 for proteasome subunit beta-5i in human RPMI8226 cells | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1182720 | Inhibition of proteasome subunit beta-2i in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1182718 | Inhibition of proteasome subunit beta-1i in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1404082 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1430564 | Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced Il-1b production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1404084 | Cytotoxicity against human fibroblasts assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1430561 | Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1404059 | Inhibition of human 20S immunoproteasome beta-1 using Ac-PAL-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1779346 | Inhibition of human trypsin-like activity of 20s proteasome beta 2i subunit using SUC-VGR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1128234 | Inhibition of beta5 subunit of immunoproteasome (unknown origin) by active-site ELISA | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates. |
| AID1779350 | Inhibition of proteasome subunit beta-5i (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1404080 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1430560 | Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNF-alpha production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1612357 | Antiinflammatory activity in human PBMC assessed as reduction in anti-CD3/CD28 antibody-stimulated IFN-gamma expression at 250 nM preincubated for 1 hr followed by anti-CD3/CD28 antibody stimulation measured after 24 hrs by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1612354 | Antiinflammatory activity in human PBMC assessed as reduction in LPS-stimulated IL-6 expression at 250 nM preincubated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1404058 | Inhibition of human 20S constitutive proteasome beta-1 using Z-LLE-betaNA as substrate incubated for 15 mins measured for 45 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. |
| AID1430536 | Inhibition of LMP2 in human MOLT4 cell lysate after 1 hr by ELISA | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1648364 | Inhibition of Beta5 in human 20S immunoproteasome usingAc-WLA-AMC as substrate after 1 hr by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
| LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease. |
| AID1779347 | Selectivity ratio of IC50 for chymotrypsin-like activity of human 20s proteasome beta 5c subunit to IC50 for human proteasome subunit beta-5i chymotrypsin like activity | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| AID1612336 | Inhibition of LMP2 in human MOLT4 cells by ELISA | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
| Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpho |
| AID1430545 | Solubility of the compound in phosphate buffer at pH 7.2 at 10 mg/ml after 24 hrs by UV-HPLC method | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4
| Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. |
| AID1182721 | Inhibition of 20s proteasome subunit beta-2c in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. |
| AID1779348 | Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of peptide epoxyketones as selective immunoproteasome inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |