Assay Detail
Binding
CHEMBL5147935
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rabbit stomach K+ stimulated H(+)/K(+) ATPase activity incubated for 30 mins in presence of ATP and KCl by malachite green reagent based assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Stomach |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of novel 5-methyl-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives as potent potassium-competitive acid blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.24 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2079130 | VONOPRAZAN | 4.0 | 1 | 7.31 |
| CHEMBL5202573 | — | — | 1 | 7.22 |
| CHEMBL5193723 | — | — | 1 | 7.11 |
| CHEMBL5178383 | — | — | 1 | 7.01 |
| CHEMBL5195081 | — | — | 1 | 6.98 |
| CHEMBL5192683 | — | — | 1 | 6.89 |
| CHEMBL5173361 | — | — | 1 | 6.85 |
| CHEMBL5208167 | — | — | 1 | 6.54 |
| CHEMBL5178421 | — | — | 1 | 6.50 |
| CHEMBL5174112 | — | — | 1 | 6.49 |
| CHEMBL5175355 | — | — | 1 | 6.47 |
| CHEMBL5189639 | — | — | 1 | 6.47 |
| CHEMBL5173698 | — | — | 1 | 6.45 |
| CHEMBL5184059 | — | — | 1 | 6.42 |
| CHEMBL5200828 | — | — | 1 | 6.41 |
| CHEMBL5171989 | — | — | 1 | 6.40 |
| CHEMBL5178930 | — | — | 1 | 6.39 |
| CHEMBL5208883 | — | — | 1 | 6.38 |
| CHEMBL5183991 | — | — | 1 | 6.36 |
| CHEMBL5207851 | — | — | 1 | 6.31 |
| CHEMBL5200922 | — | — | 1 | 6.23 |
| CHEMBL5190379 | — | — | 1 | 6.17 |
| CHEMBL5196868 | — | — | 1 | 6.13 |
| CHEMBL5185909 | — | — | 1 | 6.09 |
| CHEMBL5179600 | — | — | 1 | 6.07 |
| CHEMBL5202259 | — | — | 1 | 6.05 |
| CHEMBL5197558 | — | — | 1 | 5.99 |
| CHEMBL5190526 | — | — | 1 | 5.96 |
| CHEMBL5204343 | — | — | 1 | 5.91 |
| CHEMBL5173776 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2079130 | VONOPRAZAN | IC50 | = | 49.1 | nM | 7.31 |
| CHEMBL5202573 | — | IC50 | = | 60.5 | nM | 7.22 |
| CHEMBL5193723 | — | IC50 | = | 77.3 | nM | 7.11 |
| CHEMBL5178383 | — | IC50 | = | 97.5 | nM | 7.01 |
| CHEMBL5195081 | — | IC50 | = | 104.1 | nM | 6.98 |
| CHEMBL5192683 | — | IC50 | = | 129.3 | nM | 6.89 |
| CHEMBL5173361 | — | IC50 | = | 140.4 | nM | 6.85 |
| CHEMBL5208167 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5178421 | — | IC50 | = | 313.1 | nM | 6.50 |
| CHEMBL5174112 | — | IC50 | = | 327.7 | nM | 6.49 |
| CHEMBL5175355 | — | IC50 | = | 339.5 | nM | 6.47 |
| CHEMBL5189639 | — | IC50 | = | 342.2 | nM | 6.47 |
| CHEMBL5173698 | — | IC50 | = | 354.5 | nM | 6.45 |
| CHEMBL5184059 | — | IC50 | = | 375.9 | nM | 6.42 |
| CHEMBL5200828 | — | IC50 | = | 388.9 | nM | 6.41 |
| CHEMBL5171989 | — | IC50 | = | 396.1 | nM | 6.40 |
| CHEMBL5178930 | — | IC50 | = | 410.5 | nM | 6.39 |
| CHEMBL5208883 | — | IC50 | = | 415.6 | nM | 6.38 |
| CHEMBL5183991 | — | IC50 | = | 440.5 | nM | 6.36 |
| CHEMBL5207851 | — | IC50 | = | 488.5 | nM | 6.31 |
| CHEMBL5200922 | — | IC50 | = | 584.7 | nM | 6.23 |
| CHEMBL5190379 | — | IC50 | = | 674.0 | nM | 6.17 |
| CHEMBL5196868 | — | IC50 | = | 746.8 | nM | 6.13 |
| CHEMBL5185909 | — | IC50 | = | 814.2 | nM | 6.09 |
| CHEMBL5179600 | — | IC50 | = | 861.0 | nM | 6.07 |
| CHEMBL5202259 | — | IC50 | = | 894.0 | nM | 6.05 |
| CHEMBL5197558 | — | IC50 | = | 1031.0 | nM | 5.99 |
| CHEMBL5190526 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5204343 | — | IC50 | = | 1239.0 | nM | 5.91 |
| CHEMBL5173776 | — | IC50 | = | 1839.0 | nM | 5.74 |
| CHEMBL5207911 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL5188539 | — | IC50 | = | 2108.0 | nM | 5.68 |
| CHEMBL5190406 | — | IC50 | = | 2161.0 | nM | 5.67 |
| CHEMBL5179860 | — | IC50 | = | 3203.0 | nM | 5.49 |
| CHEMBL5192776 | — | IC50 | = | 3582.0 | nM | 5.45 |
| CHEMBL5205348 | — | IC50 | = | 4168.0 | nM | 5.38 |
| CHEMBL5188776 | — | IC50 | = | 4305.0 | nM | 5.37 |
| CHEMBL5189950 | — | IC50 | = | 6354.0 | nM | 5.20 |
| CHEMBL5181111 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5184081 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5204781 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5176130 | — | IC50 | > | 10000.0 | nM | - |