Assay Detail
Binding
CHEMBL5733730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FGFR Family Enzymatic Activity Assay: A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kinase activity of a compound of Formula (III). Serial dilutions of test compounds were incubated with either human recombinant FGFR1 (0.5 nM), FGFR2 (0.1 nM, FGFR3 (0.9 nM), or FGFR4 (2 nM), ATP (FGFR1: 100 μM; FGFR2: 75 μM; FGFR3: 120 μM; FGFR4: 250 μM) and a phosphoacceptor peptide substrate FAM-KKKKEEIYFFF-CONH2 (1 μM) at room temperature for 3 h. The reaction was then terminated with EDTA, final concentration 20 mM and the phosphorylated reaction product was quantified on a Caliper LabChip 3000. Percent inhibition was calculated for each compound dilution and the concentration that produced 50% inhibition was calculated. This value is presented as the IC50.
318
Total Activities
106
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Quinolone derivatives as fibroblast growth factor receptor inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 106 | 8.64 | 10.00 |
| kon | 106 | - | - |
| k_off | 106 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5951244 | — | — | 3 | 10.00 |
| CHEMBL6008228 | — | — | 3 | 9.52 |
| CHEMBL6030761 | — | — | 3 | 9.40 |
| CHEMBL4099992 | — | — | 3 | 9.40 |
| CHEMBL4068509 | PRN-1371 | 1.0 | 3 | 9.22 |
| CHEMBL6022837 | — | — | 3 | 9.22 |
| CHEMBL4061766 | — | — | 3 | 9.15 |
| CHEMBL5782310 | — | — | 3 | 9.15 |
| CHEMBL5882059 | — | — | 3 | 9.15 |
| CHEMBL5876465 | — | — | 3 | 9.15 |
| CHEMBL5958998 | — | — | 3 | 9.10 |
| CHEMBL5979626 | — | — | 3 | 9.10 |
| CHEMBL5932759 | — | — | 3 | 9.05 |
| CHEMBL5892171 | — | — | 3 | 9.05 |
| CHEMBL5883166 | — | — | 3 | 9.05 |
| CHEMBL6005296 | — | — | 3 | 9.05 |
| CHEMBL6060451 | — | — | 3 | 9.05 |
| CHEMBL5911670 | — | — | 3 | 9.05 |
| CHEMBL5998134 | — | — | 3 | 9.00 |
| CHEMBL5743270 | — | — | 3 | 9.00 |
| CHEMBL6019639 | — | — | 3 | 8.96 |
| CHEMBL5912688 | — | — | 3 | 8.96 |
| CHEMBL5832330 | — | — | 3 | 8.96 |
| CHEMBL5816550 | — | — | 3 | 8.96 |
| CHEMBL5957332 | — | — | 3 | 8.96 |
| CHEMBL5867788 | — | — | 3 | 8.92 |
| CHEMBL6007821 | — | — | 3 | 8.92 |
| CHEMBL5893335 | — | — | 3 | 8.92 |
| CHEMBL5884080 | — | — | 3 | 8.92 |
| CHEMBL6022862 | — | — | 3 | 8.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5951244 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL6008228 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL6030761 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4099992 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL6022837 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4068509 | PRN-1371 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4061766 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5882059 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5782310 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5876465 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5979626 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5958998 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5911670 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL6005296 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL6060451 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5932759 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5892171 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5883166 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5743270 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5998134 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5957332 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5816550 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5832330 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6019639 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5912688 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6007821 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5884080 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5893335 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5867788 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL6022862 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5976388 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5918455 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5926912 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5931467 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5836220 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5836062 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL6038718 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5912864 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4095844 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5746066 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5966033 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL6060670 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5743421 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL6064162 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL6033282 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL6058905 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL6053846 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5955323 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5917299 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5827768 | — | IC50 | = | 1.8 | nM | 8.74 |