Assay Detail
Binding
CHEMBL3888717
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences).
35
Total Activities
23
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 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.09 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3909470 | — | — | 2 | 7.82 |
| CHEMBL3951994 | — | — | 6 | 7.82 |
| CHEMBL3913959 | — | — | 2 | 7.80 |
| CHEMBL3952996 | — | — | 1 | 7.77 |
| CHEMBL3904195 | — | — | 1 | 7.70 |
| CHEMBL3901913 | — | — | 3 | 7.68 |
| CHEMBL3947915 | — | — | 1 | 7.64 |
| CHEMBL3915145 | — | — | 1 | 7.43 |
| CHEMBL3986396 | — | — | 1 | 7.36 |
| CHEMBL3979652 | — | — | 3 | 7.28 |
| CHEMBL3956601 | — | — | 1 | 7.16 |
| CHEMBL3935902 | — | — | 2 | 7.10 |
| CHEMBL3934321 | — | — | 1 | 7.08 |
| CHEMBL3906175 | — | — | 1 | 6.97 |
| CHEMBL3976863 | — | — | 1 | 6.96 |
| CHEMBL3902863 | — | — | 1 | 6.94 |
| CHEMBL3980279 | — | — | 1 | 6.77 |
| CHEMBL4106677 | — | — | 1 | 6.75 |
| CHEMBL3891755 | — | — | 1 | 6.71 |
| CHEMBL3900726 | — | — | 1 | 6.66 |
| CHEMBL3963336 | — | — | 1 | 6.53 |
| CHEMBL3968340 | — | — | 1 | 6.01 |
| CHEMBL3956663 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3909470 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3951994 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3913959 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3952996 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3904195 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3901913 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3947915 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3901913 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3951994 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3915145 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3986396 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3909470 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3979652 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3951994 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3956601 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3935902 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3934321 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3901913 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3979652 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3979652 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3906175 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3976863 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL3902863 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3951994 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3951994 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL3935902 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3980279 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4106677 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL3891755 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL3900726 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL3913959 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL3951994 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL3963336 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL3968340 | — | IC50 | = | 982.0 | nM | 6.01 |
| CHEMBL3956663 | — | IC50 | = | 1253.0 | nM | 5.90 |