Assay Detail
Binding
CHEMBL3887674
Review assay metadata, readout intent, target linkage, and publication context from the same page.
High ATP Kinase Assay: For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio-One, Frickenhausen, Germany) 2 μl of a solution of the above FGFR-1 fusion protein in aqueous assay buffer [8 mM MOPS pH 7.0, 10 mM magnesium acetate, 1.0 mM dithiothreitol, 0.05% (w/v) bovine serum albumin (BSA), 0.07% (v/v) Tween-20, 0.2 mM EDTA] was added, and the mixture was incubated for 15 min at 22° C. to allow pre-binding of the test compound to the enzyme. Then, the kinase reaction was started by the addition of 3 ul of a solution of adenosine triphosphate (ATP, 3.3 mM; final concentration in the 5 ul assay volume=2 mM) and substrate (0.16 uM; final concentration in the 5 ul assay volume=0.1 uM) in assay buffer, and the resulting mixture was incubated for a reaction time of 15 min at 22° C. The concentration of FGFR-1 fusion protein was adjusted depending on the activity of the enzyme lot.
123
Total Activities
115
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Disubstituted benzothienyl-pyrrolotriazines and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 123 | 8.19 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3951786 | — | — | 1 | 9.30 |
| CHEMBL3924399 | — | — | 2 | 9.30 |
| CHEMBL3909132 | — | — | 1 | 9.15 |
| CHEMBL3892887 | — | — | 1 | 9.05 |
| CHEMBL3895503 | — | — | 1 | 9.05 |
| CHEMBL3979384 | — | — | 1 | 9.05 |
| CHEMBL3985178 | — | — | 1 | 9.00 |
| CHEMBL3926373 | — | — | 1 | 9.00 |
| CHEMBL3934668 | — | — | 1 | 9.00 |
| CHEMBL3905236 | — | — | 1 | 8.96 |
| CHEMBL3907995 | — | — | 1 | 8.89 |
| CHEMBL3918062 | — | — | 1 | 8.89 |
| CHEMBL3937124 | — | — | 1 | 8.89 |
| CHEMBL3906839 | — | — | 2 | 8.85 |
| CHEMBL3929322 | — | — | 1 | 8.85 |
| CHEMBL3938823 | — | — | 1 | 8.85 |
| CHEMBL3938826 | — | — | 1 | 8.82 |
| CHEMBL3889953 | — | — | 1 | 8.80 |
| CHEMBL3938513 | — | — | 1 | 8.80 |
| CHEMBL3952635 | — | — | 1 | 8.77 |
| CHEMBL3911335 | — | — | 2 | 8.72 |
| CHEMBL3984301 | — | — | 1 | 8.68 |
| CHEMBL3929725 | — | — | 1 | 8.68 |
| CHEMBL3969060 | — | — | 1 | 8.68 |
| CHEMBL4108692 | — | — | 1 | 8.62 |
| CHEMBL3914307 | — | — | 1 | 8.60 |
| CHEMBL3897839 | — | — | 1 | 8.57 |
| CHEMBL3958993 | — | — | 1 | 8.55 |
| CHEMBL3906882 | — | — | 1 | 8.55 |
| CHEMBL3943773 | — | — | 1 | 8.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3924399 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3951786 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3909132 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3924399 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3892887 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3895503 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3979384 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3934668 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3985178 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3926373 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3905236 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3937124 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3918062 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3907995 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3929322 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3906839 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3938823 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3938826 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3938513 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3889953 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3906839 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3952635 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3911335 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3969060 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3984301 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3929725 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4108692 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3914307 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3897839 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3943773 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3958993 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3906882 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3948716 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3924079 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3949626 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3930377 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3929808 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3907380 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3911335 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3944496 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3948076 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3954561 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3897224 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3944881 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3953385 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3949665 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3920417 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3919371 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4106638 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3923490 | — | IC50 | = | 4.2 | nM | 8.38 |