Assay Detail
Binding
CHEMBL5100326
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Inhibition of recombinant human FGFR3 V555M mutant using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
7
Total Activities
7
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
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.76 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5184953 | — | — | 1 | 9.05 |
| CHEMBL5187371 | — | — | 1 | 8.49 |
| CHEMBL5203027 | — | — | 1 | 8.28 |
| CHEMBL5180631 | — | — | 1 | 8.21 |
| CHEMBL5189383 | — | — | 1 | 7.17 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 6.70 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5184953 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5187371 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5203027 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5180631 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5189383 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 352.0 | nM | 6.45 |