Assay Detail
Binding
CHEMBL5129937
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Inhibition of CXCR3 receptor internalization in human venous whole blood incubated for 30 mins by flow cytometer analysis
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 49 | 6.46 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5177520 | — | — | 1 | 7.60 |
| CHEMBL5172352 | — | — | 1 | 7.54 |
| CHEMBL5177288 | — | — | 1 | 7.35 |
| CHEMBL5169888 | — | — | 1 | 7.33 |
| CHEMBL5172053 | — | — | 1 | 7.32 |
| CHEMBL5186627 | — | — | 1 | 7.22 |
| CHEMBL3978935 | — | — | 1 | 7.16 |
| CHEMBL5187464 | — | — | 1 | 7.05 |
| CHEMBL5186167 | — | — | 1 | 6.99 |
| CHEMBL5197065 | — | — | 1 | 6.98 |
| CHEMBL5181928 | — | — | 1 | 6.80 |
| CHEMBL5192156 | — | — | 1 | 6.74 |
| CHEMBL5185762 | — | — | 1 | 6.72 |
| CHEMBL5202301 | — | — | 1 | 6.69 |
| CHEMBL5175118 | — | — | 1 | 6.67 |
| CHEMBL5183256 | — | — | 1 | 6.64 |
| CHEMBL5193432 | — | — | 1 | 6.61 |
| CHEMBL5198351 | — | — | 1 | 6.57 |
| CHEMBL5190681 | — | — | 1 | 6.54 |
| CHEMBL5203452 | — | — | 1 | 6.51 |
| CHEMBL5206539 | — | — | 1 | 6.45 |
| CHEMBL5190588 | — | — | 1 | 6.44 |
| CHEMBL5193608 | — | — | 1 | 6.43 |
| CHEMBL5195689 | — | — | 1 | 6.43 |
| CHEMBL5208823 | — | — | 1 | 6.42 |
| CHEMBL3971056 | — | — | 1 | 6.28 |
| CHEMBL5197175 | — | — | 1 | 6.28 |
| CHEMBL5200240 | — | — | 1 | 6.27 |
| CHEMBL3918205 | — | — | 1 | 6.26 |
| CHEMBL3895485 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5177520 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5172352 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5177288 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5169888 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5172053 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5186627 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3978935 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5187464 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5186167 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5197065 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5181928 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5192156 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL5185762 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5202301 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL5175118 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL5183256 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5193432 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL5198351 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5190681 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL5203452 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL5206539 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL5190588 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL5193608 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL5195689 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL5208823 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL5197175 | — | IC50 | = | 524.0 | nM | 6.28 |
| CHEMBL3971056 | — | IC50 | = | 526.0 | nM | 6.28 |
| CHEMBL5200240 | — | IC50 | = | 536.0 | nM | 6.27 |
| CHEMBL3918205 | — | IC50 | = | 554.0 | nM | 6.26 |
| CHEMBL3895485 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL5183818 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL5192208 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5205683 | — | IC50 | = | 674.0 | nM | 6.17 |
| CHEMBL5197253 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL5201967 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3917322 | — | IC50 | = | 851.0 | nM | 6.07 |
| CHEMBL5208280 | — | IC50 | = | 887.0 | nM | 6.05 |
| CHEMBL3919018 | — | IC50 | = | 994.0 | nM | 6.00 |
| CHEMBL5181086 | — | IC50 | = | 1043.0 | nM | 5.98 |
| CHEMBL3966706 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL3945976 | — | IC50 | = | 1154.0 | nM | 5.94 |
| CHEMBL3927250 | — | IC50 | = | 1154.0 | nM | 5.94 |
| CHEMBL5183171 | — | IC50 | = | 1158.0 | nM | 5.94 |
| CHEMBL5194504 | — | IC50 | = | 1192.0 | nM | 5.92 |
| CHEMBL3925131 | — | IC50 | = | 1437.0 | nM | 5.84 |
| CHEMBL5181702 | — | IC50 | = | 1575.0 | nM | 5.80 |
| CHEMBL3931920 | — | IC50 | = | 2468.0 | nM | 5.61 |
| CHEMBL3957343 | — | IC50 | = | 3381.0 | nM | 5.47 |
| CHEMBL5205299 | — | IC50 | > | 21000.0 | nM | - |