Assay Detail
Functional
CHEMBL5054302
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Antitumour activity against human JJN3R cells measured after 72 hrs by MTS assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | JJN-3R |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.99 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080354 | — | — | 1 | 8.51 |
| CHEMBL5082474 | — | — | 1 | 8.51 |
| CHEMBL4297458 | EZOBRESIB | 2.0 | 1 | 8.44 |
| CHEMBL5087175 | — | — | 1 | 8.08 |
| CHEMBL5093440 | — | — | 1 | 7.96 |
| CHEMBL3786449 | — | — | 1 | 7.46 |
| CHEMBL5074438 | — | — | 1 | 7.42 |
| CHEMBL5075046 | — | — | 1 | 7.34 |
| CHEMBL5074708 | — | — | 1 | 7.02 |
| CHEMBL5075119 | — | — | 1 | 6.89 |
| CHEMBL5094725 | — | — | 1 | 6.38 |
| CHEMBL5090216 | — | — | 1 | 6.38 |
| CHEMBL5089900 | — | — | 1 | 6.28 |
| CHEMBL5085106 | — | — | 1 | 6.10 |
| CHEMBL5080617 | — | — | 1 | 5.53 |
| CHEMBL5093519 | — | — | 1 | 5.45 |
| CHEMBL5090264 | — | — | 1 | 5.12 |
| CHEMBL5083442 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080354 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5082474 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4297458 | EZOBRESIB | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5087175 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5093440 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3786449 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5074438 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5075046 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5074708 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5075119 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5094725 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL5090216 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL5089900 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL5085106 | — | IC50 | = | 796.0 | nM | 6.10 |
| CHEMBL5080617 | — | IC50 | = | 2962.0 | nM | 5.53 |
| CHEMBL5093519 | — | IC50 | = | 3527.0 | nM | 5.45 |
| CHEMBL5090264 | — | IC50 | = | 7596.0 | nM | 5.12 |
| CHEMBL5083442 | — | IC50 | > | 2500.0 | nM | - |