Assay Detail
Binding
CHEMBL891341
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Inhibition of calcium channel Cav2.2 in IMR32 cells
41
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent N-type calcium channel subunit alpha-1B (CHEMBL4478) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 5.84 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL231820 | — | — | 1 | 6.68 |
| CHEMBL232849 | — | — | 2 | 6.36 |
| CHEMBL245173 | — | — | 1 | 6.31 |
| CHEMBL389993 | — | — | 1 | 6.30 |
| CHEMBL233855 | — | — | 1 | 6.29 |
| CHEMBL234915 | — | — | 1 | 6.28 |
| CHEMBL268157 | — | — | 1 | 6.25 |
| CHEMBL234490 | — | — | 1 | 6.24 |
| CHEMBL234914 | — | — | 1 | 6.23 |
| CHEMBL245171 | — | — | 1 | 6.22 |
| CHEMBL232032 | — | — | 1 | 6.20 |
| CHEMBL234938 | — | — | 1 | 6.18 |
| CHEMBL231799 | — | — | 1 | 6.16 |
| CHEMBL398158 | — | — | 2 | 6.11 |
| CHEMBL243019 | — | — | 1 | 6.06 |
| CHEMBL389103 | — | — | 1 | 5.97 |
| CHEMBL234943 | — | — | 1 | 5.90 |
| CHEMBL234510 | — | — | 1 | 5.89 |
| CHEMBL395982 | — | — | 1 | 5.89 |
| CHEMBL395109 | — | — | 1 | 5.89 |
| CHEMBL412849 | — | — | 1 | 5.88 |
| CHEMBL232848 | — | — | 1 | 5.88 |
| CHEMBL390705 | — | — | 1 | 5.87 |
| CHEMBL234916 | — | — | 1 | 5.86 |
| CHEMBL234698 | — | — | 1 | 5.85 |
| CHEMBL390703 | — | — | 1 | 5.78 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 1 | 5.78 |
| CHEMBL398157 | — | — | 1 | 5.71 |
| CHEMBL390704 | — | — | 1 | 5.62 |
| CHEMBL29188 | LOMERIZINE | 2.0 | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL231820 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL232849 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL245173 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL389993 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL233855 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL234915 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL268157 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL234490 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL234914 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL245171 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL232032 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL234938 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL231799 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL232849 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL398158 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL243019 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL389103 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL234943 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL395109 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL234510 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL395982 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL232848 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL412849 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL390705 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL234916 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL234698 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL390703 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL398157 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL390704 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL29188 | LOMERIZINE | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL398158 | — | IC50 | = | 3320.0 | nM | 5.48 |
| CHEMBL232034 | — | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL234273 | — | IC50 | = | 3970.0 | nM | 5.40 |
| CHEMBL234491 | — | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL234274 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL394578 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL234511 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL231826 | — | IC50 | = | 8930.0 | nM | 5.05 |
| CHEMBL390187 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL234719 | — | IC50 | = | 29800.0 | nM | 4.53 |