Assay Detail
Binding
CHEMBL2434720
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Inhibition of Escherichia coli TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 5.73 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2431997 | — | — | 1 | 6.75 |
| CHEMBL2432012 | — | — | 1 | 6.72 |
| CHEMBL2432016 | — | — | 1 | 6.54 |
| CHEMBL2432022 | — | — | 1 | 6.48 |
| CHEMBL2432013 | — | — | 1 | 6.48 |
| CHEMBL2432021 | — | — | 1 | 6.40 |
| CHEMBL2432017 | — | — | 1 | 6.40 |
| CHEMBL2432015 | — | — | 1 | 6.38 |
| CHEMBL2431996 | — | — | 1 | 6.36 |
| CHEMBL2432010 | — | — | 1 | 6.36 |
| CHEMBL2432020 | — | — | 1 | 6.33 |
| CHEMBL2432011 | — | — | 1 | 6.28 |
| CHEMBL2432014 | — | — | 1 | 6.17 |
| CHEMBL2432006 | — | — | 1 | 6.05 |
| CHEMBL2432009 | — | — | 1 | 6.05 |
| CHEMBL2432018 | — | — | 1 | 6.05 |
| CHEMBL2432000 | — | — | 1 | 6.04 |
| CHEMBL2432007 | — | — | 1 | 6.00 |
| CHEMBL2432008 | — | — | 1 | 5.89 |
| CHEMBL2432001 | — | — | 1 | 5.75 |
| CHEMBL2432029 | — | — | 1 | 5.64 |
| CHEMBL2432019 | — | — | 1 | 5.55 |
| CHEMBL2432005 | — | — | 1 | 5.33 |
| CHEMBL2432023 | — | — | 1 | 5.32 |
| CHEMBL2432002 | — | — | 1 | 5.31 |
| CHEMBL2432003 | — | — | 1 | 5.23 |
| CHEMBL2432033 | — | — | 1 | 5.19 |
| CHEMBL1427554 | — | — | 1 | 5.16 |
| CHEMBL1214186 | SINEFUNGIN | 2.0 | 1 | 4.96 |
| CHEMBL2432035 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2431997 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2432012 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2432016 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2432022 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2432013 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2432021 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2432017 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2432015 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2431996 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2432010 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2432020 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2432011 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL2432014 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL2432018 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL2432009 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL2432006 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2432000 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL2432007 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2432008 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2432001 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2432029 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2432019 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2432005 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2432023 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2432002 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2432003 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2432033 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1427554 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL1214186 | SINEFUNGIN | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2432035 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1369722 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2432036 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2432004 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2432030 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL2432027 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL2431999 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2432031 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2432032 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2432028 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL2432026 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2432025 | — | IC50 | - | — | - | |
| CHEMBL2432034 | — | IC50 | = | 139000.0 | nM | - |
| CHEMBL2432037 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2431998 | — | IC50 | = | 123000.0 | nM | - |