Assay Detail
Binding
CHEMBL3888716
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).
34
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 34 | 6.43 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3913959 | — | — | 2 | 7.70 |
| CHEMBL3952996 | — | — | 1 | 7.52 |
| CHEMBL3909470 | — | — | 2 | 7.44 |
| CHEMBL3904195 | — | — | 1 | 7.38 |
| CHEMBL3901913 | — | — | 3 | 7.37 |
| CHEMBL3951994 | — | — | 6 | 7.36 |
| CHEMBL3935902 | — | — | 2 | 7.05 |
| CHEMBL3956601 | — | — | 1 | 6.95 |
| CHEMBL3915145 | — | — | 1 | 6.77 |
| CHEMBL3979652 | — | — | 3 | 6.61 |
| CHEMBL3986396 | — | — | 1 | 6.42 |
| CHEMBL3934321 | — | — | 1 | 6.32 |
| CHEMBL3902863 | — | — | 1 | 6.29 |
| CHEMBL3891755 | — | — | 1 | 6.26 |
| CHEMBL3947915 | — | — | 1 | 6.19 |
| CHEMBL3906175 | — | — | 1 | 6.15 |
| CHEMBL3900726 | — | — | 1 | 6.09 |
| CHEMBL3980279 | — | — | 1 | 5.94 |
| CHEMBL4106677 | — | — | 1 | 5.88 |
| CHEMBL3976863 | — | — | 1 | 5.72 |
| CHEMBL3963336 | — | — | 1 | 5.42 |
| CHEMBL3968340 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3913959 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3952996 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3909470 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3904195 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3901913 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3951994 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3951994 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3909470 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3935902 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3901913 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL3956601 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL3915145 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3979652 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL3986396 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL3934321 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL3902863 | — | IC50 | = | 508.0 | nM | 6.29 |
| CHEMBL3891755 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL3935902 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3947915 | — | IC50 | = | 652.0 | nM | 6.19 |
| CHEMBL3951994 | — | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL3951994 | — | IC50 | = | 692.0 | nM | 6.16 |
| CHEMBL3906175 | — | IC50 | = | 711.0 | nM | 6.15 |
| CHEMBL3979652 | — | IC50 | = | 819.0 | nM | 6.09 |
| CHEMBL3900726 | — | IC50 | = | 812.0 | nM | 6.09 |
| CHEMBL3901913 | — | IC50 | = | 859.0 | nM | 6.07 |
| CHEMBL3913959 | — | IC50 | = | 1096.0 | nM | 5.96 |
| CHEMBL3980279 | — | IC50 | = | 1148.0 | nM | 5.94 |
| CHEMBL4106677 | — | IC50 | = | 1322.0 | nM | 5.88 |
| CHEMBL3951994 | — | IC50 | = | 1564.0 | nM | 5.81 |
| CHEMBL3976863 | — | IC50 | = | 1892.0 | nM | 5.72 |
| CHEMBL3979652 | — | IC50 | = | 2075.0 | nM | 5.68 |
| CHEMBL3963336 | — | IC50 | = | 3808.0 | nM | 5.42 |
| CHEMBL3951994 | — | IC50 | = | 4554.0 | nM | 5.34 |
| CHEMBL3968340 | — | IC50 | = | 8907.0 | nM | 5.05 |