Assay Detail
Binding
CHEMBL3404248
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Inhibition of FGFR1 (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 | 5.60 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3348846 | FEXAGRATINIB | 2.0 | 1 | 8.89 |
| CHEMBL3401358 | — | — | 1 | 7.09 |
| CHEMBL57366 | — | — | 1 | 6.96 |
| CHEMBL3401370 | — | — | 1 | 5.81 |
| CHEMBL3401369 | — | — | 1 | 5.50 |
| CHEMBL3401364 | — | — | 1 | 5.32 |
| CHEMBL3401363 | — | — | 1 | 5.27 |
| CHEMBL3401367 | — | — | 1 | 5.04 |
| CHEMBL3401368 | — | — | 1 | 5.02 |
| CHEMBL3401361 | — | — | 1 | 4.92 |
| CHEMBL3401362 | — | — | 1 | 4.90 |
| CHEMBL3401366 | — | — | 1 | 4.82 |
| CHEMBL3401360 | — | — | 1 | 4.82 |
| CHEMBL3401359 | — | — | 1 | 4.82 |
| CHEMBL3401365 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3348846 | FEXAGRATINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3401358 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL57366 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3401370 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL3401369 | — | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL3401364 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL3401363 | — | IC50 | = | 5330.0 | nM | 5.27 |
| CHEMBL3401367 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL3401368 | — | IC50 | = | 9590.0 | nM | 5.02 |
| CHEMBL3401361 | — | IC50 | = | 11910.0 | nM | 4.92 |
| CHEMBL3401362 | — | IC50 | = | 12650.0 | nM | 4.90 |
| CHEMBL3401366 | — | IC50 | = | 15040.0 | nM | 4.82 |
| CHEMBL3401360 | — | IC50 | = | 15220.0 | nM | 4.82 |
| CHEMBL3401359 | — | IC50 | = | 15180.0 | nM | 4.82 |
| CHEMBL3401365 | — | IC50 | = | 17840.0 | nM | 4.75 |