Assay Detail
Binding
CHEMBL3404249
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Inhibition of FGFR2 (unknown origin) after 90 mins by TR-FRET assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.49 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3348846 | FEXAGRATINIB | 2.0 | 1 | 8.49 |
| CHEMBL3401358 | — | — | 1 | 7.20 |
| CHEMBL57366 | — | — | 1 | 6.89 |
| CHEMBL3401370 | — | — | 1 | 5.21 |
| CHEMBL3401367 | — | — | 1 | 5.20 |
| CHEMBL3401369 | — | — | 1 | 5.12 |
| CHEMBL3401361 | — | — | 1 | 5.08 |
| CHEMBL3401368 | — | — | 1 | 5.04 |
| CHEMBL3401364 | — | — | 1 | 5.04 |
| CHEMBL3401363 | — | — | 1 | 5.02 |
| CHEMBL3401366 | — | — | 1 | 4.87 |
| CHEMBL3401359 | — | — | 1 | 4.87 |
| CHEMBL3401360 | — | — | 1 | 4.80 |
| CHEMBL3401365 | — | — | 1 | 4.79 |
| CHEMBL3401362 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3348846 | FEXAGRATINIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3401358 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL57366 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3401370 | — | IC50 | = | 6140.0 | nM | 5.21 |
| CHEMBL3401367 | — | IC50 | = | 6280.0 | nM | 5.20 |
| CHEMBL3401369 | — | IC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL3401361 | — | IC50 | = | 8390.0 | nM | 5.08 |
| CHEMBL3401368 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL3401364 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL3401363 | — | IC50 | = | 9580.0 | nM | 5.02 |
| CHEMBL3401366 | — | IC50 | = | 13470.0 | nM | 4.87 |
| CHEMBL3401359 | — | IC50 | = | 13460.0 | nM | 4.87 |
| CHEMBL3401360 | — | IC50 | = | 15730.0 | nM | 4.80 |
| CHEMBL3401365 | — | IC50 | = | 16110.0 | nM | 4.79 |
| CHEMBL3401362 | — | IC50 | = | 17710.0 | nM | 4.75 |