Assay Detail
Functional
CHEMBL2184682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human alpha3beta4 nAChR expressed in CHO cells assessed as calcium flux by calcium4-based FLIPR assay
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 60 | 4.66 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179962 | — | — | 1 | 5.92 |
| CHEMBL2179964 | — | — | 1 | 5.85 |
| CHEMBL2179965 | — | — | 1 | 5.75 |
| CHEMBL2179554 | — | — | 1 | 5.40 |
| CHEMBL2179963 | — | — | 1 | 5.38 |
| CHEMBL2179961 | — | — | 1 | 5.31 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 5.16 |
| CHEMBL2179968 | — | — | 1 | 5.16 |
| CHEMBL2179557 | — | — | 1 | 5.16 |
| CHEMBL2179540 | — | — | 1 | 5.04 |
| CHEMBL2179525 | — | — | 1 | 5.04 |
| CHEMBL2179556 | — | — | 1 | 4.89 |
| CHEMBL2179555 | — | — | 1 | 4.85 |
| CHEMBL2179543 | — | — | 1 | 4.82 |
| CHEMBL2179970 | — | — | 1 | 4.82 |
| CHEMBL2179558 | — | — | 1 | 4.80 |
| CHEMBL2179969 | — | — | 1 | 4.77 |
| CHEMBL1876219 | — | — | 1 | 4.70 |
| CHEMBL2179551 | — | — | 1 | 4.68 |
| CHEMBL2179531 | — | — | 1 | 4.66 |
| CHEMBL2179537 | — | — | 1 | 4.66 |
| CHEMBL2179541 | — | — | 1 | 4.66 |
| CHEMBL2179539 | — | — | 1 | 4.64 |
| CHEMBL2179548 | — | — | 1 | 4.62 |
| CHEMBL2179553 | — | — | 1 | 4.60 |
| CHEMBL2179521 | — | — | 1 | 4.60 |
| CHEMBL2179534 | — | — | 1 | 4.57 |
| CHEMBL2179519 | — | — | 1 | 4.55 |
| CHEMBL2179522 | — | — | 1 | 4.55 |
| CHEMBL2179523 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179962 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2179964 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2179965 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2179554 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2179963 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2179961 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3 | NICOTINE | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2179968 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2179557 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2179540 | — | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL2179525 | — | EC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2179556 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2179555 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2179543 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2179970 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2179558 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2179969 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1876219 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2179551 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2179531 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2179537 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2179541 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2179539 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2179548 | — | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2179521 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2179553 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2179534 | — | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2179519 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2179522 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2179523 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2179545 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2179517 | — | EC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL2179532 | — | EC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL2179546 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2179520 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2179536 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2179526 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2179971 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2179542 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2179516 | — | EC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2179549 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL2179957 | — | EC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2179559 | — | EC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2179550 | — | EC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2179527 | — | EC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL2179533 | — | EC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL2179552 | — | EC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2179966 | — | EC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL2179967 | — | EC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL2179528 | — | EC50 | = | 44000.0 | nM | 4.36 |