Assay Detail
Binding
CHEMBL1954527
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Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.96 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1951914 | AZD5672 | 2.0 | 1 | 9.59 |
| CHEMBL212689 | — | — | 1 | 9.49 |
| CHEMBL1951913 | — | — | 1 | 9.36 |
| CHEMBL1951917 | — | — | 1 | 9.26 |
| CHEMBL1951912 | — | — | 1 | 9.17 |
| CHEMBL1951915 | — | — | 1 | 9.16 |
| CHEMBL1951906 | — | — | 1 | 8.96 |
| CHEMBL1951898 | — | — | 1 | 8.80 |
| CHEMBL1951907 | — | — | 1 | 8.62 |
| CHEMBL1951894 | — | — | 1 | 8.51 |
| CHEMBL1951918 | — | — | 1 | 8.46 |
| CHEMBL1951911 | — | — | 1 | 8.30 |
| CHEMBL1951893 | — | — | 1 | 8.30 |
| CHEMBL1949696 | — | — | 1 | 8.27 |
| CHEMBL1951899 | — | — | 1 | 8.05 |
| CHEMBL1951904 | — | — | 1 | 8.05 |
| CHEMBL1951897 | — | — | 1 | 7.82 |
| CHEMBL1951905 | — | — | 1 | 7.43 |
| CHEMBL1951896 | — | — | 1 | 7.41 |
| CHEMBL1951902 | — | — | 1 | 7.08 |
| CHEMBL1951903 | — | — | 1 | 6.90 |
| CHEMBL1951901 | — | — | 1 | 6.79 |
| CHEMBL1951895 | — | — | 1 | 6.64 |
| CHEMBL1951900 | — | — | 1 | 6.47 |
| CHEMBL1951892 | — | — | 1 | 6.44 |
| CHEMBL1951910 | — | — | 1 | 6.10 |
| CHEMBL1951909 | — | — | 1 | 5.43 |
| CHEMBL1951916 | — | — | 1 | - |
| CHEMBL1951908 | — | — | 1 | - |
| CHEMBL1952100 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1951914 | AZD5672 | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL212689 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1951913 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL1951917 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL1951912 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL1951915 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL1951906 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1951898 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1951907 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1951894 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL1951918 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1951911 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1951893 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1949696 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1951899 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL1951904 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL1951897 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1951905 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1951896 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1951902 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1951903 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL1951901 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL1951895 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL1951900 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL1951892 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL1951910 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL1951909 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1951916 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL1951908 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL1952100 | — | IC50 | < | 0.1 | nM | - |