Assay Detail
Binding
CHEMBL5100324
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human FGFR3 V555L 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
8
Total Activities
8
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 | 8 | 7.64 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5200643 | — | — | 1 | 9.30 |
| CHEMBL5184953 | — | — | 1 | 8.59 |
| CHEMBL5187371 | — | — | 1 | 8.28 |
| CHEMBL5189383 | — | — | 1 | 7.68 |
| CHEMBL5180631 | — | — | 1 | 7.68 |
| CHEMBL5189074 | — | — | 1 | 7.66 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 6.43 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5200643 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5184953 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5187371 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5189383 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5180631 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5189074 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 3036.0 | nM | 5.52 |