Assay Detail
Binding
CHEMBL2339600
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Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB2 Receptor Inverse Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 7.10 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381689 | SR-144528 | — | 1 | 8.68 |
| CHEMBL2336549 | — | — | 1 | 8.40 |
| CHEMBL2336543 | — | — | 1 | 8.27 |
| CHEMBL2336538 | — | — | 1 | 8.26 |
| CHEMBL2336536 | — | — | 1 | 8.02 |
| CHEMBL2336537 | — | — | 1 | 7.85 |
| CHEMBL2336540 | — | — | 1 | 7.85 |
| CHEMBL2336539 | — | — | 1 | 7.75 |
| CHEMBL2336545 | — | — | 1 | 7.70 |
| CHEMBL2336544 | — | — | 1 | 7.52 |
| CHEMBL2336546 | — | — | 1 | 7.51 |
| CHEMBL2336528 | — | — | 1 | 7.50 |
| CHEMBL2336535 | — | — | 1 | 7.47 |
| CHEMBL2336541 | — | — | 1 | 7.44 |
| CHEMBL2336552 | — | — | 1 | 7.36 |
| CHEMBL2336566 | — | — | 1 | 7.34 |
| CHEMBL2336573 | — | — | 1 | 7.28 |
| CHEMBL2336548 | — | — | 1 | 7.26 |
| CHEMBL2336542 | — | — | 1 | 7.18 |
| CHEMBL2336565 | — | — | 1 | 7.15 |
| CHEMBL2336561 | — | — | 1 | 7.14 |
| CHEMBL2336547 | — | — | 1 | 7.12 |
| CHEMBL2336567 | — | — | 1 | 7.03 |
| CHEMBL2336562 | — | — | 1 | 6.99 |
| CHEMBL2336534 | — | — | 1 | 6.92 |
| CHEMBL2336530 | — | — | 1 | 6.92 |
| CHEMBL2336555 | — | — | 1 | 6.89 |
| CHEMBL2336556 | — | — | 1 | 6.89 |
| CHEMBL2336529 | — | — | 1 | 6.85 |
| CHEMBL2336559 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381689 | SR-144528 | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2336549 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2336543 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2336538 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL2336536 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL2336537 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2336540 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2336539 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2336545 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2336544 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2336546 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2336528 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2336535 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2336541 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL2336552 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2336566 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2336573 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL2336548 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2336542 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2336565 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL2336561 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2336547 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2336567 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL2336562 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL2336534 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2336530 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2336555 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2336556 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2336529 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2336559 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2336570 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL2336551 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL2336563 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2336553 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL2336569 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL2336532 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2336558 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL2336554 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL2336560 | — | Ki | = | 262.0 | nM | 6.58 |
| CHEMBL2336557 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL2336527 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL2336533 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL2336564 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL2336531 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL2336568 | — | Ki | = | 577.0 | nM | 6.24 |
| CHEMBL2336550 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL2336571 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL111 | RIMONABANT | Ki | - | — | - |