Assay Detail
Binding
CHEMBL4059167
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mAChR in human CCRF-CEM cells assessed as decrease in acetylacholine-stimulated Ca2+ flux preincubated for 25 mins followed by acetylacholine addition measured for 90 secs by calcium dye-based fluorescence assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 4.99 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096305 | — | — | 1 | 6.22 |
| CHEMBL4084920 | — | — | 1 | 5.92 |
| CHEMBL4098635 | — | — | 1 | 5.61 |
| CHEMBL4062981 | — | — | 1 | 5.46 |
| CHEMBL4075205 | — | — | 1 | 5.25 |
| CHEMBL4094123 | — | — | 1 | 5.16 |
| CHEMBL4072645 | — | — | 1 | 5.16 |
| CHEMBL4061381 | — | — | 1 | 5.06 |
| CHEMBL4081338 | — | — | 1 | 4.94 |
| CHEMBL4105591 | — | — | 1 | 4.94 |
| CHEMBL4065224 | — | — | 1 | 4.94 |
| CHEMBL4083122 | — | — | 1 | 4.91 |
| CHEMBL4086739 | — | — | 1 | 4.89 |
| CHEMBL4073818 | — | — | 1 | 4.89 |
| CHEMBL4094400 | — | — | 1 | 4.73 |
| CHEMBL4086662 | — | — | 1 | 4.73 |
| CHEMBL4071612 | — | — | 1 | 4.70 |
| CHEMBL4059462 | — | — | 1 | 4.70 |
| CHEMBL4070320 | — | — | 1 | 4.70 |
| CHEMBL4099550 | — | — | 1 | 4.67 |
| CHEMBL4081958 | — | — | 1 | 4.66 |
| CHEMBL4075694 | — | — | 1 | 4.59 |
| CHEMBL4062223 | — | — | 1 | 4.55 |
| CHEMBL4066459 | — | — | 1 | 4.46 |
| CHEMBL4076841 | — | — | 1 | - |
| CHEMBL4089531 | — | — | 1 | - |
| CHEMBL4074366 | — | — | 1 | - |
| CHEMBL4101106 | — | — | 1 | - |
| CHEMBL4084652 | — | — | 1 | - |
| CHEMBL4092405 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096305 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL4084920 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4098635 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL4062981 | — | IC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL4075205 | — | IC50 | = | 5610.0 | nM | 5.25 |
| CHEMBL4094123 | — | IC50 | = | 6980.0 | nM | 5.16 |
| CHEMBL4072645 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL4061381 | — | IC50 | = | 8760.0 | nM | 5.06 |
| CHEMBL4081338 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL4105591 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4065224 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL4083122 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL4086739 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL4073818 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4086662 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL4094400 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL4070320 | — | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL4071612 | — | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL4059462 | — | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL4099550 | — | IC50 | = | 21400.0 | nM | 4.67 |
| CHEMBL4081958 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4075694 | — | IC50 | = | 25700.0 | nM | 4.59 |
| CHEMBL4062223 | — | IC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL4066459 | — | IC50 | = | 35100.0 | nM | 4.46 |
| CHEMBL4068122 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4059622 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4080718 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4104948 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4104056 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4086147 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4070843 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4078260 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4097946 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4081436 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4089307 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4090235 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4088588 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4065751 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL3091687 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4082134 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL3091683 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4090772 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4092405 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4084652 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4101106 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4074366 | — | IC50 | > | 33300.0 | nM | - |
| CHEMBL4089531 | — | IC50 | > | 16700.0 | nM | - |
| CHEMBL4076841 | — | IC50 | > | 16700.0 | nM | - |