Assay Detail
Functional
CHEMBL4144846
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Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CCRF-CEM |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.54 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159607 | — | — | 1 | 7.50 |
| CHEMBL4096305 | — | — | 1 | 6.21 |
| CHEMBL4161528 | — | — | 1 | 6.11 |
| CHEMBL4164075 | — | — | 1 | 5.96 |
| CHEMBL4175500 | — | — | 1 | 5.06 |
| CHEMBL4174727 | — | — | 1 | 5.02 |
| CHEMBL4167221 | — | — | 1 | 5.00 |
| CHEMBL4164874 | — | — | 1 | 4.96 |
| CHEMBL4163770 | — | — | 2 | 4.89 |
| CHEMBL4167521 | — | — | 1 | 4.64 |
| CHEMBL4086147 | — | — | 1 | - |
| CHEMBL4169450 | — | — | 1 | - |
| CHEMBL4160401 | — | — | 1 | - |
| CHEMBL4171643 | — | — | 1 | - |
| CHEMBL4175088 | — | — | 1 | - |
| CHEMBL4161850 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159607 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4096305 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4161528 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4164075 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4175500 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4174727 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4167221 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4164874 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4163770 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4167521 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4161850 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4175088 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4171643 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4163770 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4160401 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL4169450 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL4086147 | — | IC50 | > | 16000.0 | nM | - |