Assay Detail
Functional
CHEMBL3583382
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 42 | 8.23 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3582344 | — | — | 1 | 9.52 |
| CHEMBL3582339 | — | — | 1 | 9.40 |
| CHEMBL3582321 | — | — | 1 | 9.40 |
| CHEMBL3582342 | — | — | 1 | 9.30 |
| CHEMBL3582329 | — | — | 1 | 9.15 |
| CHEMBL3582343 | — | — | 1 | 9.10 |
| CHEMBL3582335 | — | — | 1 | 9.10 |
| CHEMBL2204935 | — | — | 1 | 9.05 |
| CHEMBL3582340 | — | — | 1 | 9.00 |
| CHEMBL3582336 | — | — | 1 | 8.96 |
| CHEMBL3582320 | — | — | 1 | 8.92 |
| CHEMBL3582319 | — | — | 1 | 8.92 |
| CHEMBL3582341 | — | — | 1 | 8.89 |
| CHEMBL3580681 | — | — | 1 | 8.80 |
| CHEMBL3582331 | — | — | 1 | 8.66 |
| CHEMBL3323086 | — | — | 1 | 8.62 |
| CHEMBL3582317 | — | — | 1 | 8.60 |
| CHEMBL3582328 | — | — | 1 | 8.48 |
| CHEMBL3582327 | — | — | 1 | 8.46 |
| CHEMBL3582334 | — | — | 1 | 8.35 |
| CHEMBL3582332 | — | — | 1 | 8.33 |
| CHEMBL3582326 | — | — | 1 | 8.32 |
| CHEMBL3582316 | — | — | 1 | 8.32 |
| CHEMBL3582325 | — | — | 1 | 8.29 |
| CHEMBL3582330 | — | — | 1 | 8.28 |
| CHEMBL3582324 | — | — | 1 | 8.16 |
| CHEMBL3582318 | — | — | 1 | 7.96 |
| CHEMBL3582323 | — | — | 1 | 7.96 |
| CHEMBL3582311 | — | — | 1 | 7.88 |
| CHEMBL3582307 | — | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3582344 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3582339 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3582321 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3582342 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3582329 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3582343 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3582335 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2204935 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3582340 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3582336 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3582320 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3582319 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3582341 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3580681 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3582331 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3323086 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3582317 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3582328 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3582327 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3582334 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3582332 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3582326 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3582316 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3582325 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3582330 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3582324 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3582318 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3582323 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL3582311 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL3582307 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3582310 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL3582314 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL3582333 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL2069500 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL3582312 | — | IC50 | = | 28.1 | nM | 7.55 |
| CHEMBL3582313 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL3582338 | — | IC50 | = | 75.4 | nM | 7.12 |
| CHEMBL3582315 | — | IC50 | = | 134.6 | nM | 6.87 |
| CHEMBL3582337 | — | IC50 | = | 137.9 | nM | 6.86 |
| CHEMBL3582309 | — | IC50 | = | 156.6 | nM | 6.80 |
| CHEMBL3582308 | — | IC50 | = | 538.6 | nM | 6.27 |
| CHEMBL3582322 | — | IC50 | = | 1948.0 | nM | 5.71 |