Assay Detail
Functional
CHEMBL5129938
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and <i>In Vivo</i> Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 6.61 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5172053 | — | — | 1 | 7.70 |
| CHEMBL5177520 | — | — | 1 | 7.64 |
| CHEMBL5172352 | — | — | 1 | 7.62 |
| CHEMBL3978935 | — | — | 1 | 7.51 |
| CHEMBL5177288 | — | — | 1 | 7.48 |
| CHEMBL5169888 | — | — | 1 | 7.33 |
| CHEMBL5185762 | — | — | 1 | 7.31 |
| CHEMBL5193608 | — | — | 1 | 7.26 |
| CHEMBL5186167 | — | — | 1 | 7.16 |
| CHEMBL5203452 | — | — | 1 | 7.11 |
| CHEMBL5186627 | — | — | 1 | 7.06 |
| CHEMBL5187464 | — | — | 1 | 7.03 |
| CHEMBL5200240 | — | — | 1 | 7.00 |
| CHEMBL5198351 | — | — | 1 | 6.98 |
| CHEMBL5197175 | — | — | 1 | 6.93 |
| CHEMBL3971056 | — | — | 1 | 6.90 |
| CHEMBL5194504 | — | — | 1 | 6.88 |
| CHEMBL5175118 | — | — | 1 | 6.86 |
| CHEMBL5208823 | — | — | 1 | 6.85 |
| CHEMBL5190681 | — | — | 1 | 6.79 |
| CHEMBL5197065 | — | — | 1 | 6.78 |
| CHEMBL5190588 | — | — | 1 | 6.76 |
| CHEMBL5181928 | — | — | 1 | 6.75 |
| CHEMBL5202301 | — | — | 1 | 6.65 |
| CHEMBL5195689 | — | — | 1 | 6.59 |
| CHEMBL5193432 | — | — | 1 | 6.57 |
| CHEMBL5192156 | — | — | 1 | 6.49 |
| CHEMBL5205683 | — | — | 1 | 6.46 |
| CHEMBL5208280 | — | — | 1 | 6.30 |
| CHEMBL5206539 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5172053 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5177520 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5172352 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3978935 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5177288 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5169888 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5185762 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5193608 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5186167 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5203452 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5186627 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5187464 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5200240 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5198351 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5197175 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3971056 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5194504 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5175118 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5208823 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5190681 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL5197065 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5190588 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5181928 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL5202301 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL5195689 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL5193432 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL5192156 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL5205683 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL5208280 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL5206539 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL5181086 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL5192208 | — | IC50 | = | 578.0 | nM | 6.24 |
| CHEMBL5201967 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL3931920 | — | IC50 | = | 599.0 | nM | 6.22 |
| CHEMBL3917322 | — | IC50 | = | 604.0 | nM | 6.22 |
| CHEMBL3919018 | — | IC50 | = | 745.0 | nM | 6.13 |
| CHEMBL5177069 | — | IC50 | = | 811.0 | nM | 6.09 |
| CHEMBL3918205 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3895485 | — | IC50 | = | 862.0 | nM | 6.06 |
| CHEMBL5183171 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL3966706 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL5181702 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL5183818 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL3945976 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL3927250 | — | IC50 | = | 6220.0 | nM | 5.21 |
| CHEMBL3894991 | — | IC50 | = | 8030.0 | nM | 5.09 |
| CHEMBL3957343 | — | IC50 | > | 10000.0 | nM | - |