Assay Detail
Binding
CHEMBL2167992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ADAMTS-5 expressed in CHO cells using WAAG-3R as substrate preincubated for 15 mins measured after 1 hr by FRET assay
54
Total Activities
54
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 |
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 (CHEMBL2285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 6.32 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187092 | — | — | 1 | 8.20 |
| CHEMBL2164094 | — | — | 1 | 7.52 |
| CHEMBL2164121 | — | — | 1 | 7.52 |
| CHEMBL2164122 | — | — | 1 | 7.40 |
| CHEMBL2164107 | — | — | 1 | 7.30 |
| CHEMBL2164120 | — | — | 1 | 7.30 |
| CHEMBL2163735 | — | — | 1 | 7.30 |
| CHEMBL2164117 | — | — | 1 | 7.22 |
| CHEMBL2164111 | — | — | 1 | 7.16 |
| CHEMBL2164113 | — | — | 1 | 7.05 |
| CHEMBL2164103 | — | — | 1 | 6.96 |
| CHEMBL2164109 | — | — | 1 | 6.92 |
| CHEMBL2164115 | — | — | 1 | 6.68 |
| CHEMBL2163736 | — | — | 1 | 6.64 |
| CHEMBL2164449 | — | — | 1 | 6.62 |
| CHEMBL2164114 | — | — | 1 | 6.58 |
| CHEMBL2164104 | — | — | 1 | 6.41 |
| CHEMBL2164092 | — | — | 1 | 6.39 |
| CHEMBL2164087 | — | — | 1 | 6.37 |
| CHEMBL2163738 | — | — | 1 | 6.34 |
| CHEMBL2164078 | — | — | 1 | 6.16 |
| CHEMBL2164079 | — | — | 1 | 6.14 |
| CHEMBL2164088 | — | — | 1 | 6.06 |
| CHEMBL2164089 | — | — | 1 | 5.93 |
| CHEMBL2164080 | — | — | 1 | 5.90 |
| CHEMBL2164084 | — | — | 1 | 5.82 |
| CHEMBL2164099 | — | — | 1 | 5.81 |
| CHEMBL2164112 | — | — | 1 | 5.80 |
| CHEMBL2164085 | — | — | 1 | 5.80 |
| CHEMBL2164082 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187092 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2164094 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2164121 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2164122 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2164107 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2164120 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2163735 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2164117 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2164111 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2164113 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2164103 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2164109 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2164115 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2163736 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2164449 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2164114 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2164104 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2164092 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2164087 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2163738 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2164078 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2164079 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2164088 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL2164089 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL2164080 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL2164084 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2164099 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL2164112 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2164085 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2164082 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2164116 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL2164086 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2164106 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2164110 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2164083 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2164091 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2164081 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2164105 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2164098 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2164097 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2164100 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2163737 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164123 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164448 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2163734 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164102 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164101 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164118 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164108 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164096 | — | IC50 | > | 10000.0 | nM | - |