Assay Detail
Functional
CHEMBL5130041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 8.11 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3917642 | — | — | 1 | 8.80 |
| CHEMBL3978935 | — | — | 1 | 8.80 |
| CHEMBL3924716 | — | — | 1 | 8.77 |
| CHEMBL3914555 | — | — | 1 | 8.70 |
| CHEMBL3966250 | — | — | 1 | 8.68 |
| CHEMBL3976317 | — | — | 1 | 8.66 |
| CHEMBL3980161 | — | — | 1 | 8.60 |
| CHEMBL3985006 | — | — | 1 | 8.59 |
| CHEMBL3913741 | — | — | 1 | 8.57 |
| CHEMBL3973196 | — | — | 1 | 8.55 |
| CHEMBL5190291 | — | — | 1 | 8.51 |
| CHEMBL5179941 | — | — | 1 | 8.51 |
| CHEMBL3892103 | — | — | 1 | 8.51 |
| CHEMBL3908818 | — | — | 1 | 8.49 |
| CHEMBL3927485 | — | — | 1 | 8.49 |
| CHEMBL3981151 | — | — | 1 | 8.48 |
| CHEMBL3955848 | — | — | 1 | 8.44 |
| CHEMBL5200180 | — | — | 1 | 8.44 |
| CHEMBL5183995 | — | — | 1 | 8.44 |
| CHEMBL3982035 | — | — | 1 | 8.42 |
| CHEMBL5193975 | — | — | 1 | 8.41 |
| CHEMBL3949824 | — | — | 1 | 8.34 |
| CHEMBL3979234 | — | — | 1 | 8.24 |
| CHEMBL3940550 | — | — | 1 | 8.24 |
| CHEMBL3903412 | — | — | 1 | 8.22 |
| CHEMBL3970456 | — | — | 1 | 8.21 |
| CHEMBL5174313 | — | — | 1 | 8.03 |
| CHEMBL5193530 | — | — | 1 | 8.00 |
| CHEMBL3982804 | — | — | 1 | 7.89 |
| CHEMBL3926820 | — | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3917642 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3978935 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3924716 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3914555 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3966250 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3976317 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3980161 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3985006 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3913741 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3973196 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5179941 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3892103 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5190291 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3908818 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3927485 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3981151 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3955848 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5200180 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5183995 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3982035 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5193975 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3949824 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3979234 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3940550 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3903412 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3970456 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5174313 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5193530 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3982804 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3926820 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5192187 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3938074 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3901607 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5183078 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5198121 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3899775 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3944489 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5192464 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5203982 | — | IC50 | = | 2100.0 | nM | 5.68 |