Assay Detail
Binding
CHEMBL3583383
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Inhibition of MK499 binding to human ERG
42
Total Activities
42
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.26 | 7.05 |
| Ki | 6 | 6.50 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3582308 | — | — | 1 | 7.30 |
| CHEMBL2069500 | — | — | 1 | 7.10 |
| CHEMBL3582314 | — | — | 1 | 7.05 |
| CHEMBL3582316 | — | — | 1 | 6.77 |
| CHEMBL3582313 | — | — | 1 | 6.72 |
| CHEMBL3582312 | — | — | 1 | 6.70 |
| CHEMBL3582307 | — | — | 1 | 6.54 |
| CHEMBL3582315 | — | — | 1 | 6.47 |
| CHEMBL3582309 | — | — | 1 | 6.36 |
| CHEMBL3582311 | — | — | 1 | 6.14 |
| CHEMBL3582331 | — | — | 1 | 5.96 |
| CHEMBL3582322 | — | — | 1 | 5.92 |
| CHEMBL3582329 | — | — | 1 | 5.80 |
| CHEMBL2204935 | — | — | 1 | 5.77 |
| CHEMBL3582310 | — | — | 1 | 5.54 |
| CHEMBL3582324 | — | — | 1 | 5.50 |
| CHEMBL3582321 | — | — | 1 | 5.50 |
| CHEMBL3582342 | — | — | 1 | 5.47 |
| CHEMBL3582323 | — | — | 1 | 5.43 |
| CHEMBL3582318 | — | — | 1 | 5.38 |
| CHEMBL3582325 | — | — | 1 | 5.37 |
| CHEMBL3582341 | — | — | 1 | 5.26 |
| CHEMBL3582332 | — | — | 1 | 5.26 |
| CHEMBL3582319 | — | — | 1 | 5.14 |
| CHEMBL3582340 | — | — | 1 | 5.11 |
| CHEMBL3582339 | — | — | 1 | 5.11 |
| CHEMBL3582317 | — | — | 1 | 5.07 |
| CHEMBL3582326 | — | — | 1 | 5.07 |
| CHEMBL3582320 | — | — | 1 | 5.02 |
| CHEMBL3582328 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3582308 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2069500 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL3582314 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3582316 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3582313 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3582312 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3582307 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL3582315 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3582309 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL3582311 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL3582331 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3582322 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3582329 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2204935 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3582310 | — | Ki | = | 2870.0 | nM | 5.54 |
| CHEMBL3582324 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3582321 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3582342 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3582323 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3582318 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3582325 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3582341 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3582332 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3582319 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL3582340 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3582339 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3582317 | — | IC50 | = | 8540.0 | nM | 5.07 |
| CHEMBL3582326 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL3582320 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3582328 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL3582333 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL3582327 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL3582334 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL3582338 | — | IC50 | = | 27100.0 | nM | 4.57 |
| CHEMBL3582335 | — | IC50 | = | 27900.0 | nM | 4.55 |
| CHEMBL3582343 | — | IC50 | = | 30500.0 | nM | 4.52 |
| CHEMBL3582336 | — | IC50 | = | 32200.0 | nM | 4.49 |
| CHEMBL3582344 | — | IC50 | = | 34500.0 | nM | 4.46 |
| CHEMBL3582330 | — | IC50 | = | 35400.0 | nM | 4.45 |
| CHEMBL3582337 | — | IC50 | = | 39900.0 | nM | 4.40 |
| CHEMBL3580681 | — | IC50 | = | 51500.0 | nM | 4.29 |
| CHEMBL3323086 | — | IC50 | = | 95600.0 | nM | 4.02 |