Assay Detail
Binding
CHEMBL1049024
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Displacement of 125I-IP10 from recombinant human CXCR3 receptor expressed in Ba/F3 cell membrane after 1 to 4 hrs by scintillation counting
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Novel CXCR3 antagonists with a piperazinyl-piperidine core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.26 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL570734 | — | — | 1 | 7.80 |
| CHEMBL569117 | — | — | 1 | 7.50 |
| CHEMBL578779 | — | — | 1 | 7.46 |
| CHEMBL565760 | — | — | 1 | 7.16 |
| CHEMBL578546 | — | — | 1 | 7.07 |
| CHEMBL571377 | — | — | 1 | 7.07 |
| CHEMBL565980 | — | — | 1 | 7.05 |
| CHEMBL568676 | — | — | 1 | 6.96 |
| CHEMBL565970 | — | — | 1 | 6.92 |
| CHEMBL577409 | — | — | 1 | 6.85 |
| CHEMBL568668 | — | — | 1 | 6.80 |
| CHEMBL570356 | — | — | 1 | 6.50 |
| CHEMBL583655 | — | — | 1 | 6.48 |
| CHEMBL579195 | — | — | 1 | 6.43 |
| CHEMBL565968 | — | — | 1 | 6.39 |
| CHEMBL576841 | — | — | 1 | 6.33 |
| CHEMBL571289 | — | — | 1 | 6.29 |
| CHEMBL565761 | — | — | 1 | 6.25 |
| CHEMBL583651 | — | — | 1 | 6.06 |
| CHEMBL565559 | — | — | 1 | 5.72 |
| CHEMBL584079 | — | — | 1 | 5.72 |
| CHEMBL569336 | — | — | 1 | 5.70 |
| CHEMBL570958 | — | — | 1 | 5.57 |
| CHEMBL571467 | — | — | 1 | 5.54 |
| CHEMBL565979 | — | — | 1 | 5.43 |
| CHEMBL576842 | — | — | 1 | 5.42 |
| CHEMBL587391 | — | — | 1 | 5.39 |
| CHEMBL570509 | — | — | 1 | 5.35 |
| CHEMBL570705 | — | — | 1 | 5.14 |
| CHEMBL587013 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL570734 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL569117 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL578779 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL565760 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL578546 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL571377 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL565980 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL568676 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL565970 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL577409 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL568668 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL570356 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL583655 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL579195 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL565968 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL576841 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL571289 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL565761 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL583651 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL565559 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL584079 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL569336 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL570958 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL571467 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL565979 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL576842 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL587391 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL570509 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL570705 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL587013 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL571815 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL568684 | — | Ki | > | 50000.0 | nM | - |