Assay Detail
Binding
CHEMBL4136605
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Inhibition of Mycobacterium tuberculosis PknB (M1 to G279 residues) expressed in Escherichia coli BL21 (DE3) cells using [T-33P]ATP as substrate after 50 mins in presence of GarA by liquid scintillation method
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase PknB (CHEMBL1908385) ↗| Type | SINGLE PROTEIN |
| Organism | Mycobacterium tuberculosis |
Publication
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.23 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170479 | — | — | 1 | 8.40 |
| CHEMBL4173915 | — | — | 1 | 8.40 |
| CHEMBL4177229 | — | — | 1 | 8.30 |
| CHEMBL4170653 | — | — | 1 | 8.22 |
| CHEMBL4177445 | — | — | 1 | 7.89 |
| CHEMBL4165949 | — | — | 1 | 7.82 |
| CHEMBL4172982 | — | — | 1 | 7.77 |
| CHEMBL4170446 | — | — | 1 | 7.64 |
| CHEMBL4162511 | — | — | 1 | 7.64 |
| CHEMBL4162719 | — | — | 1 | 7.62 |
| CHEMBL4159344 | — | — | 1 | 7.54 |
| CHEMBL4169382 | — | — | 1 | 7.42 |
| CHEMBL4174082 | — | — | 1 | 7.40 |
| CHEMBL4166840 | — | — | 1 | 7.34 |
| CHEMBL4173877 | — | — | 1 | 7.30 |
| CHEMBL4172772 | — | — | 1 | 7.22 |
| CHEMBL4162101 | — | — | 1 | 7.14 |
| CHEMBL4159392 | — | — | 1 | 7.09 |
| CHEMBL4174513 | — | — | 1 | 7.09 |
| CHEMBL4167265 | — | — | 1 | 7.06 |
| CHEMBL4170024 | — | — | 1 | 7.01 |
| CHEMBL4166603 | — | — | 1 | 6.82 |
| CHEMBL4164081 | — | — | 1 | 6.82 |
| CHEMBL4176818 | — | — | 1 | 6.82 |
| CHEMBL4173464 | — | — | 1 | 6.72 |
| CHEMBL4162756 | — | — | 1 | 6.64 |
| CHEMBL4164260 | — | — | 1 | 6.51 |
| CHEMBL4176150 | — | — | 1 | 6.51 |
| CHEMBL4166200 | — | — | 1 | 6.02 |
| CHEMBL4174912 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170479 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4173915 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4177229 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4170653 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4177445 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4165949 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4172982 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4170446 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4162511 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4162719 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4159344 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4169382 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4174082 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4166840 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4173877 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4172772 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4162101 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL4174513 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL4159392 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL4167265 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL4170024 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4166603 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4164081 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4176818 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4173464 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL4162756 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL4176150 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4164260 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4166200 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL4174912 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL4165542 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL4165984 | — | Ki | < | 2.0 | nM | - |
| CHEMBL4176789 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL4162544 | — | Ki | < | 1.0 | nM | - |
| CHEMBL4162308 | — | Ki | < | 1.3 | nM | - |
| CHEMBL4166160 | — | Ki | < | 1.0 | nM | - |