Assay Detail
Functional
CHEMBL1273040
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human orexin 2 receptor expressed in CHO cells assessed as effect in calcium mobilization by FLIPR assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 6.84 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1272307 | SB-649868 | 2.0 | 1 | 9.40 |
| CHEMBL1271489 | — | — | 1 | 8.80 |
| CHEMBL1271490 | — | — | 1 | 8.60 |
| CHEMBL1271649 | — | — | 1 | 7.80 |
| CHEMBL1272043 | — | — | 1 | 7.50 |
| CHEMBL1271702 | — | — | 1 | 7.40 |
| CHEMBL1271650 | — | — | 1 | 7.40 |
| CHEMBL1271760 | — | — | 1 | 7.30 |
| CHEMBL1271933 | — | — | 1 | 7.20 |
| CHEMBL1271878 | — | — | 1 | 7.00 |
| CHEMBL1272150 | — | — | 1 | 7.00 |
| CHEMBL1271819 | — | — | 1 | 6.80 |
| CHEMBL1272095 | — | — | 1 | 6.80 |
| CHEMBL1271989 | — | — | 1 | 6.70 |
| CHEMBL1271990 | — | — | 1 | 6.60 |
| CHEMBL1272044 | — | — | 1 | 6.50 |
| CHEMBL1271543 | — | — | 1 | 6.40 |
| CHEMBL1272151 | — | — | 1 | 6.40 |
| CHEMBL1272308 | — | — | 1 | 6.40 |
| CHEMBL1271820 | — | — | 1 | 6.30 |
| CHEMBL1271934 | — | — | 1 | 6.30 |
| CHEMBL1271542 | — | — | 1 | 6.30 |
| CHEMBL1271491 | — | — | 1 | 6.20 |
| CHEMBL1271701 | — | — | 1 | 6.00 |
| CHEMBL1272206 | — | — | 1 | 6.00 |
| CHEMBL1272096 | — | — | 1 | 6.00 |
| CHEMBL1272205 | — | — | 1 | 5.80 |
| CHEMBL1272309 | — | — | 1 | 5.70 |
| CHEMBL1271877 | — | — | 1 | 5.70 |
| CHEMBL1271598 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1272307 | SB-649868 | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL1271489 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1271490 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL1271649 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1272043 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1271702 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1271650 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1271760 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1271933 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1271878 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1272150 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1271819 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1272095 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1271989 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1271990 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL1272044 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1272308 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1272151 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1271543 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1271820 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1271934 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1271542 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1271491 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1271701 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1272206 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1272096 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1272205 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL1272309 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL1271877 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL1271598 | — | Ki | > | 15848.93 | nM | - |
| CHEMBL1271599 | — | Ki | > | 15848.93 | nM | - |
| CHEMBL1271761 | — | Ki | > | 15848.93 | nM | - |
| CHEMBL1272259 | — | Ki | > | 15848.93 | nM | - |
| CHEMBL1272260 | — | Ki | > | 15848.93 | nM | - |