Assay Detail
Binding
CHEMBL3706135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR1 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul of FGFR1 protein (Cama Biosciences, Inc., 08-133) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 ul, of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration of 1000 nM and ATP (Promega Corporation, V9102) in a final concentration of 58.3 uM, and 5 ul of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 uL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at morn temperature for 40 minutes.
130
Total Activities
128
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
Monocyclic pyridine derivative
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 130 | 7.99 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3691333 | — | — | 1 | 8.47 |
| CHEMBL3691342 | — | — | 1 | 8.43 |
| CHEMBL3691341 | — | — | 1 | 8.41 |
| CHEMBL3691332 | — | — | 1 | 8.38 |
| CHEMBL3691334 | — | — | 1 | 8.38 |
| CHEMBL3686886 | — | — | 1 | 8.36 |
| CHEMBL3691321 | — | — | 1 | 8.30 |
| CHEMBL3691328 | — | — | 1 | 8.30 |
| CHEMBL3691336 | — | — | 1 | 8.29 |
| CHEMBL3686885 | — | — | 1 | 8.28 |
| CHEMBL3686887 | — | — | 1 | 8.28 |
| CHEMBL3691353 | — | — | 1 | 8.28 |
| CHEMBL3691262 | — | — | 2 | 8.27 |
| CHEMBL3691322 | — | — | 1 | 8.27 |
| CHEMBL3691331 | — | — | 1 | 8.27 |
| CHEMBL3691279 | — | — | 1 | 8.26 |
| CHEMBL3686882 | — | — | 1 | 8.25 |
| CHEMBL3691337 | — | — | 1 | 8.25 |
| CHEMBL3686883 | — | — | 1 | 8.24 |
| CHEMBL3686884 | E-7090 | 2.0 | 1 | 8.24 |
| CHEMBL3691319 | — | — | 1 | 8.24 |
| CHEMBL3691325 | — | — | 1 | 8.24 |
| CHEMBL3691356 | — | — | 1 | 8.21 |
| CHEMBL3691358 | — | — | 1 | 8.21 |
| CHEMBL3686888 | — | — | 1 | 8.20 |
| CHEMBL3691263 | — | — | 2 | 8.19 |
| CHEMBL3691312 | — | — | 1 | 8.19 |
| CHEMBL3691316 | — | — | 1 | 8.19 |
| CHEMBL3691354 | — | — | 1 | 8.19 |
| CHEMBL3691335 | — | — | 1 | 8.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3691333 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3691342 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3691341 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3691334 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3691332 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3686886 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3691328 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3691321 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3691336 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3691353 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3686885 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3686887 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3691322 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3691262 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3691331 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3691279 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3686882 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3691337 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3686883 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3686884 | E-7090 | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3691325 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3691319 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3691358 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3691356 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3686888 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3691354 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3691316 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3691263 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3691312 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3691262 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3691335 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3691315 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3691318 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3691311 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3691357 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3691355 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3691346 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3691320 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3691317 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3686866 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3691327 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3686865 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3691305 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3691258 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3691280 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3691310 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3691314 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3691330 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3691304 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3691352 | — | IC50 | = | 8.5 | nM | 8.07 |