Assay Detail
Functional
CHEMBL908828
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Inhibition of HCT116 cell growth
28
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.71 | 7.10 |
| IC90 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384304 | RG-547 | 2.0 | 2 | 7.10 |
| CHEMBL213713 | — | — | 1 | 6.66 |
| CHEMBL385733 | — | — | 1 | 6.52 |
| CHEMBL215086 | — | — | 1 | 6.28 |
| CHEMBL268507 | — | — | 2 | 6.19 |
| CHEMBL216126 | — | — | 1 | 5.80 |
| CHEMBL387448 | — | — | 1 | 5.68 |
| CHEMBL385190 | — | — | 1 | 5.58 |
| CHEMBL265903 | — | — | 1 | 5.47 |
| CHEMBL385907 | — | — | 1 | 5.44 |
| CHEMBL277351 | — | — | 1 | 5.44 |
| CHEMBL217443 | — | — | 1 | 5.38 |
| CHEMBL217537 | — | — | 1 | 5.30 |
| CHEMBL384356 | — | — | 1 | 5.25 |
| CHEMBL385373 | — | — | 1 | 5.16 |
| CHEMBL383875 | — | — | 1 | 4.96 |
| CHEMBL437330 | — | — | 1 | 4.78 |
| CHEMBL214433 | — | — | 1 | - |
| CHEMBL408439 | — | — | 1 | - |
| CHEMBL214831 | — | — | 1 | - |
| CHEMBL214025 | — | — | 1 | - |
| CHEMBL214183 | — | — | 1 | - |
| CHEMBL216148 | — | — | 1 | - |
| CHEMBL385039 | — | — | 1 | - |
| CHEMBL214838 | — | — | 1 | - |
| CHEMBL214458 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384304 | RG-547 | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL213713 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL385733 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL215086 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL268507 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL216126 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL387448 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL385190 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL265903 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL385907 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL277351 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL217443 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL217537 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL384356 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL385373 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL383875 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL437330 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL214433 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL214025 | — | IC50 | - | — | - | |
| CHEMBL216148 | — | IC50 | - | — | - | |
| CHEMBL214183 | — | IC50 | - | — | - | |
| CHEMBL214458 | — | IC50 | - | — | - | |
| CHEMBL214838 | — | IC50 | - | — | - | |
| CHEMBL385039 | — | IC50 | - | — | - | |
| CHEMBL214831 | — | IC50 | - | — | - | |
| CHEMBL408439 | — | IC50 | - | — | - | |
| CHEMBL384304 | RG-547 | IC90 | = | 0.075 | ug.mL-1 | - |
| CHEMBL268507 | — | IC90 | = | 0.762 | ug.mL-1 | - |