Assay ID | Title | Year | Journal | Article |
AID1687067 | Inhibition of recombinant cathepsin B (unknown origin) endopeptidase activity expressed in Escherichia coli assessed as residual activity at 100 uM using Z-RR-AMC as substrate preincubated for 30 mins under shaking in presence of 5 mM cysteine followed by | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | A road map for prioritizing warheads for cysteine targeting covalent inhibitors. |
AID699051 | Binding affinity to Mycobacterium smegmatis mc2 155 EthR assessed as protein thermal unfolding at 20 uM by SYPRO Orange dye based thermal shift assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. |
AID1160965 | Inhibition of Dengue virus serotype 2 NS2B-NS3 protease at 50 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1687064 | Inhibition of Staphylococcus aureus MurA expressed in Escherichia coli assessed as residual activity at 100 uM using UNAG and PEP as substrate preincubated for 30 mins in presence of UNAG followed by PEP addition and measured after 15 mins by malachite gr | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | A road map for prioritizing warheads for cysteine targeting covalent inhibitors. |
AID1160971 | Inhibition of wild-type Escherichia coli MurB compound preincubated for 10 mins before substrate addition at 25 uM measured after 15 mins by LC-MS method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1687069 | Inhibition of recombinant cathepsin X (unknown origin) expressed in Pichia pastoris assessed as residual activity at 100 uM using Abz-Fek(Dnp)-OH as substrate preincubated for 30 mins under shaking in presence of 5 mM cysteine followed by substrate additi | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | A road map for prioritizing warheads for cysteine targeting covalent inhibitors. |
AID1687068 | Inhibition of recombinant cathepsin B (unknown origin) exopeptidase activity expressed in Escherichia coli assessed as residual activity at 100 uM using Abz-GIVRAK(Dnp)-OH as substrate preincubated for 30 mins under shaking in presence of 5 mM cysteine fo | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | A road map for prioritizing warheads for cysteine targeting covalent inhibitors. |
AID1687066 | Inhibition of Escherichia coli MurA assessed as residual activity at 100 uM using UNAG and PEP as substrate preincubated for 30 mins in presence of UNAG followed by PEP addition and measured after 15 mins in presence of 5 mM cysteine by malachite green co | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | A road map for prioritizing warheads for cysteine targeting covalent inhibitors. |
AID1418955 | Binding affinity to recombinant C-terminal His6-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in expressed Escherichia coli Rosetta assessed as change in melting temperature by thermal shift assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL). |
AID1160969 | Inhibition of human MetAP at 25 uM after 20 mins by HPLC analysis | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160975 | Inhibition of wild-type Escherichia coli MurF compound preincubated for 10 mins before substrate addition at 25 uM measured after 15 mins by LC-MS method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160977 | Induction of covalent MurA enzyme adduct formation preincubated with UNAG substrate for 10 mins compound treated at 300 uM after 1 hr by ESI-MS analysis | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160967 | Inhibition of Bovine thrombin using Boc-Val-Pro-Arg-AMC as substrate compound preincubated at 25 uM for 15 mins by fluorescence assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160980 | Induction of covalent MetAP enzyme adduct formation at 300 uM after 1 hr by ESI-MS analysis | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160974 | Inhibition of wild-type Escherichia coli MurE compound preincubated for 10 mins before substrate addition at 25 uM measured after 15 mins by LC-MS method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160972 | Inhibition of wild-type Escherichia coli MurC compound preincubated for 10 mins before substrate addition at 25 uM measured after 15 mins by LC-MS method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160979 | Induction of covalent MurE enzyme adduct formation preincubated with UNAG substrate for 10 mins compound treated at 300 uM after 1 hr by ESI-MS analysis | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160981 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by CellTiter-Blue assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1687065 | Inhibition of Escherichia coli MurA assessed as residual activity at 100 uM using UNAG and PEP as substrate preincubated for 30 mins in presence of UNAG followed by PEP addition and measured after 15 mins by malachite green colorimetric assay relative to | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | A road map for prioritizing warheads for cysteine targeting covalent inhibitors. |
AID1160966 | Inhibition of West Nile virus NS2B-NS3 protease at 50 uM | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160973 | Inhibition of wild-type Escherichia coli MurD compound preincubated for 10 mins before substrate addition at 25 uM measured after 15 mins by LC-MS method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160970 | Inhibition of wild-type Escherichia coli MurA compound preincubated for 10 mins before substrate addition at 25 uM measured after 15 mins by LC-MS method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160976 | GSH reactivity of the compound assessed as adducts formation by RP-HPLC analysis | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
AID1160968 | Inhibition of Escherichia coli MetAP at 25 uM after 20 mins by HPLC analysis | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |