Assay Detail
Binding
CHEMBL4268770
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Mycobacterium tuberculosis recombinant N-terminal 6His-tagged HGPRT expressed in Escherichia coli BL21 (DE3) using fixed concentration of guanine and variable concentrations of PRib-PP as substrate by spectrophotometric analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Hypoxanthine-guanine phosphoribosyltransferase (CHEMBL4295584) ↗| Type | SINGLE PROTEIN |
| Organism | Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv) |
Publication
Pyrrolidine nucleoside bisphosphonates as antituberculosis agents targeting hypoxanthine-guanine phosphoribosyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.37 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4280490 | — | — | 1 | 7.40 |
| CHEMBL4290716 | — | — | 1 | 7.22 |
| CHEMBL4282830 | — | — | 1 | 7.22 |
| CHEMBL4277753 | — | — | 1 | 6.89 |
| CHEMBL4285691 | — | — | 1 | 6.70 |
| CHEMBL4291117 | — | — | 1 | 6.38 |
| CHEMBL4283940 | — | — | 1 | 5.10 |
| CHEMBL4294529 | — | — | 1 | 4.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4280490 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4290716 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4282830 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4277753 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4285691 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4291117 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL4283940 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL4294529 | — | Ki | = | 88000.0 | nM | 4.06 |