Assay Detail
Binding
CHEMBL3707937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: The in vitro affinity of the compounds of the present invention for the CXCR1 and CXCR2 receptors was determined on a functional test of the .beta.-arrestin recruitment type after receptor activation.It was demonstrated that the activation by CXCL8 of the CXCR2 receptor in cells of the PathHunter HEK293-CXCR2 line or of the CXCR1 receptor in cells of the U2OS h CXCR1 .beta.-arrestin line results in the recruitment of .beta.-arrestin (Richardson et al. 2003 Role of the cytoplasmic tails of CXCR1 and CXCR2 in mediating leukocyte migration, activation, and regulation. J. Immunol. 170: 2904-2911.)In order to evaluate the direct interaction of the CXCR2 or CXCR1 receptor with .beta.-arrestin 2, a .beta.-arrestin 2 recruitment test for CXCR2 or CXCR1 based on of .beta.-galactosidase enzyme complementation (Olson K R, Eglen R M. Beta galactosidase complementation: a cell-based luminescent assay platform for drug discovery. Assay Drug Dev Technol. 2007 February; 5(1); 137-44).
37
Total Activities
36
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
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologies
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.72 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3704565 | — | — | 1 | 7.60 |
| CHEMBL3704569 | — | — | 1 | 7.58 |
| CHEMBL3704573 | — | — | 1 | 7.52 |
| CHEMBL3701196 | — | — | 1 | 7.51 |
| CHEMBL3704564 | — | — | 2 | 7.50 |
| CHEMBL3701188 | — | — | 1 | 7.43 |
| CHEMBL3640000 | — | — | 1 | 7.22 |
| CHEMBL3704571 | — | — | 1 | 7.14 |
| CHEMBL3704570 | — | — | 1 | 7.14 |
| CHEMBL3640034 | — | — | 1 | 7.02 |
| CHEMBL3701190 | — | — | 1 | 7.00 |
| CHEMBL3701187 | — | — | 1 | 7.00 |
| CHEMBL3701184 | — | — | 1 | 6.97 |
| CHEMBL3704561 | — | — | 1 | 6.97 |
| CHEMBL3704562 | — | — | 1 | 6.84 |
| CHEMBL3704563 | — | — | 1 | 6.70 |
| CHEMBL3704555 | — | — | 1 | 6.61 |
| CHEMBL3701195 | — | — | 1 | 6.59 |
| CHEMBL3701191 | — | — | 1 | 6.58 |
| CHEMBL3701183 | — | — | 1 | 6.57 |
| CHEMBL3704568 | — | — | 1 | 6.51 |
| CHEMBL3701194 | — | — | 1 | 6.47 |
| CHEMBL3701185 | — | — | 1 | 6.47 |
| CHEMBL3704558 | — | — | 1 | 6.46 |
| CHEMBL3704572 | — | — | 1 | 6.43 |
| CHEMBL3701193 | — | — | 1 | 6.41 |
| CHEMBL3704557 | — | — | 1 | 6.36 |
| CHEMBL3704556 | — | — | 1 | 6.32 |
| CHEMBL3704567 | — | — | 1 | 6.30 |
| CHEMBL3701189 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3704565 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3704569 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3704573 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3701196 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3704564 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3701188 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3640000 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3704571 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3704570 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3640034 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3701190 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3701187 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3701184 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3704561 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3704562 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL3704563 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL3704564 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3704555 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL3701195 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL3701191 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL3701183 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL3704568 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL3701194 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL3701185 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL3704558 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL3704572 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL3701193 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL3704557 | — | IC50 | = | 433.0 | nM | 6.36 |
| CHEMBL3704556 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL3704567 | — | IC50 | = | 502.0 | nM | 6.30 |
| CHEMBL3701189 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL3701192 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL3704559 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL3704574 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL3704560 | — | IC50 | = | 962.0 | nM | 6.02 |
| CHEMBL3704566 | — | IC50 | = | 1035.0 | nM | 5.99 |
| CHEMBL3701186 | — | IC50 | = | 1088.0 | nM | 5.96 |