Assay Detail
Functional
CHEMBL5130042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Venous blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Pharmacological Evaluation of Benzimidazolo-thiazoles as Potent CXCR3 Antagonists with Therapeutic Potential in Autoimmune Diseases: Discovery of ACT-672125.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.36 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3973196 | — | — | 1 | 7.42 |
| CHEMBL3978935 | — | — | 1 | 7.16 |
| CHEMBL3914555 | — | — | 1 | 7.07 |
| CHEMBL3949824 | — | — | 1 | 7.03 |
| CHEMBL3966250 | — | — | 1 | 7.00 |
| CHEMBL3981151 | — | — | 1 | 6.91 |
| CHEMBL3917642 | — | — | 1 | 6.91 |
| CHEMBL3955848 | — | — | 1 | 6.87 |
| CHEMBL3927485 | — | — | 1 | 6.84 |
| CHEMBL3985006 | — | — | 1 | 6.84 |
| CHEMBL3982804 | — | — | 1 | 6.72 |
| CHEMBL5200180 | — | — | 1 | 6.66 |
| CHEMBL3908818 | — | — | 1 | 6.62 |
| CHEMBL3980161 | — | — | 1 | 6.62 |
| CHEMBL3924716 | — | — | 1 | 6.60 |
| CHEMBL3976317 | — | — | 1 | 6.51 |
| CHEMBL5190291 | — | — | 1 | 6.51 |
| CHEMBL3892103 | — | — | 1 | 6.49 |
| CHEMBL3913741 | — | — | 1 | 6.48 |
| CHEMBL5183995 | — | — | 1 | 6.48 |
| CHEMBL3979234 | — | — | 1 | 6.43 |
| CHEMBL5179941 | — | — | 1 | 6.42 |
| CHEMBL5193975 | — | — | 1 | 6.37 |
| CHEMBL3938074 | — | — | 1 | 6.30 |
| CHEMBL3982035 | — | — | 1 | 6.24 |
| CHEMBL5174313 | — | — | 1 | 6.20 |
| CHEMBL3903412 | — | — | 1 | 6.13 |
| CHEMBL3970456 | — | — | 1 | 6.09 |
| CHEMBL5193530 | — | — | 1 | 6.02 |
| CHEMBL3940550 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3973196 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL3978935 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3914555 | — | IC50 | = | 84.7 | nM | 7.07 |
| CHEMBL3949824 | — | IC50 | = | 92.4 | nM | 7.03 |
| CHEMBL3966250 | — | IC50 | = | 99.1 | nM | 7.00 |
| CHEMBL3981151 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3917642 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3955848 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3927485 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3985006 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL3982804 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL5200180 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3908818 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL3980161 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL3924716 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL3976317 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL5190291 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL3892103 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL5183995 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL3913741 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3979234 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL5179941 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL5193975 | — | IC50 | = | 426.0 | nM | 6.37 |
| CHEMBL3938074 | — | IC50 | = | 502.0 | nM | 6.30 |
| CHEMBL3982035 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5174313 | — | IC50 | = | 628.0 | nM | 6.20 |
| CHEMBL3903412 | — | IC50 | = | 747.0 | nM | 6.13 |
| CHEMBL3970456 | — | IC50 | = | 805.0 | nM | 6.09 |
| CHEMBL5193530 | — | IC50 | = | 959.0 | nM | 6.02 |
| CHEMBL3940550 | — | IC50 | = | 1135.0 | nM | 5.95 |
| CHEMBL5192464 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5198121 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL3926820 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL5192187 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL3901607 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL5183078 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL3899775 | — | IC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL5203982 | — | IC50 | = | 5570.0 | nM | 5.25 |
| CHEMBL3944489 | — | IC50 | = | 6890.0 | nM | 5.16 |