Assay Detail
Binding
CHEMBL3887741
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cell Activity Inhibition Assay: To check the B-Raf cell activity inhibitory capability of the compounds of the present invention, the following experiments were conducted in A375P cell line (ATCC). The A375P cell line (ATCC) was derived from a patient with human melanoma, and had V600E mutant of B-Raf gene. A375 cell was maintained in DMEM supplemented with 10% fetal bovine serum, glutamine (2 mM), penicillin (100 U/mL), and streptomycin (100 ug/mL). The cell was maintained at 37° C., and in 5% CO2 and 100% humidity. To conduct the growth inhibition test, the cell was plated by using a white 384-well microplate, with 1000 cells/20 μl plated per 1 well. After 24 hours, 5 ul of 5x stock solution of drug was added. All the drugs were initially prepared with 200x stock solution in DMSO, and the final concentration of DMSO was 0.5%. The cell was incubated at 37° C. for 72 hours. For MTT assay, 'CellTiter 96 (R) Non-Radioactive Cell Proliferation Assay (G4100)â¿¿ kit by Promega Corp. was used.
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A375P |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 44 | 6.22 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354844 | — | — | 1 | 8.70 |
| CHEMBL3944643 | — | — | 1 | 8.22 |
| CHEMBL3798780 | — | — | 1 | 7.52 |
| CHEMBL3982836 | — | — | 1 | 7.40 |
| CHEMBL3970384 | — | — | 1 | 7.22 |
| CHEMBL3798195 | — | — | 1 | 7.16 |
| CHEMBL3908401 | — | — | 1 | 7.00 |
| CHEMBL3798327 | — | — | 1 | 6.92 |
| CHEMBL3912288 | — | — | 1 | 6.82 |
| CHEMBL3798308 | — | — | 1 | 6.80 |
| CHEMBL3925705 | — | — | 1 | 6.70 |
| CHEMBL3964313 | — | — | 1 | 6.64 |
| CHEMBL3799241 | — | — | 1 | 6.60 |
| CHEMBL3798357 | — | — | 1 | 6.51 |
| CHEMBL3953209 | — | — | 1 | 6.48 |
| CHEMBL3799451 | — | — | 1 | 6.47 |
| CHEMBL3799996 | — | — | 1 | 6.44 |
| CHEMBL3921943 | — | — | 1 | 6.36 |
| CHEMBL3921326 | — | — | 1 | 6.30 |
| CHEMBL3977844 | — | — | 1 | 6.22 |
| CHEMBL3962572 | — | — | 1 | 6.17 |
| CHEMBL3935693 | — | — | 1 | 6.16 |
| CHEMBL3926427 | — | — | 1 | 6.16 |
| CHEMBL3958972 | — | — | 1 | 6.14 |
| CHEMBL3920877 | — | — | 1 | 6.12 |
| CHEMBL3958648 | — | — | 1 | 6.11 |
| CHEMBL3940852 | — | — | 1 | 6.10 |
| CHEMBL3968823 | — | — | 1 | 6.09 |
| CHEMBL3931834 | — | — | 1 | 6.00 |
| CHEMBL3799568 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354844 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3944643 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3798780 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3982836 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3970384 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3798195 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3908401 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3798327 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3912288 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3798308 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3925705 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3964313 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3799241 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3798357 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3953209 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3799451 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3799996 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3921943 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3921326 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3977844 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3962572 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3926427 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3935693 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3958972 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3920877 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3958648 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3940852 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3968823 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3931834 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3799568 | — | EC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL3892867 | — | EC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL3980306 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3893840 | — | EC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL3906265 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3954787 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3980569 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3942148 | — | EC50 | = | 5870.0 | nM | 5.23 |
| CHEMBL3935697 | — | EC50 | = | 7190.0 | nM | 5.14 |
| CHEMBL3936955 | — | EC50 | = | 8370.0 | nM | 5.08 |
| CHEMBL3902214 | — | EC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3930284 | — | EC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL3963766 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3968811 | — | EC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL3986093 | — | EC50 | > | 15000.0 | nM | - |