Assay Detail
Functional
CHEMBL5355535
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as inhibition of fenoterol-induced CRE-SPAP production by measuring rightward shift of the fenoterol concentration response curve measured after 5 hrs incubation
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rational design, synthesis, and pharmacological evaluation of a cohort of novel beta-adrenergic receptors ligands enables an assessment of structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 34 | 6.11 | 8.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL280822 | CGP-20712A | — | 1 | 8.99 |
| CHEMBL1326499 | — | — | 1 | 7.43 |
| CHEMBL5427527 | — | — | 1 | 6.99 |
| CHEMBL513389 | ZENIDOLOL | 2.0 | 1 | 6.92 |
| CHEMBL5397120 | — | — | 1 | 6.87 |
| CHEMBL5430355 | — | — | 1 | 6.59 |
| CHEMBL4238084 | — | — | 1 | 6.47 |
| CHEMBL5415148 | — | — | 1 | 5.80 |
| CHEMBL5428413 | — | — | 1 | 5.78 |
| CHEMBL5416996 | — | — | 1 | 5.76 |
| CHEMBL5431834 | — | — | 1 | 5.64 |
| CHEMBL5422259 | — | — | 1 | 5.62 |
| CHEMBL5395772 | — | — | 1 | 5.51 |
| CHEMBL5432691 | — | — | 1 | 5.50 |
| CHEMBL5437540 | — | — | 1 | 5.49 |
| CHEMBL5423415 | — | — | 1 | 5.44 |
| CHEMBL5432967 | — | — | 1 | 5.44 |
| CHEMBL5426087 | — | — | 1 | 5.41 |
| CHEMBL5430136 | — | — | 1 | 5.25 |
| CHEMBL5402516 | — | — | 1 | 5.22 |
| CHEMBL5434276 | — | — | 1 | - |
| CHEMBL5395675 | — | — | 1 | - |
| CHEMBL5416424 | — | — | 1 | - |
| CHEMBL5413563 | — | — | 1 | - |
| CHEMBL5403431 | — | — | 1 | - |
| CHEMBL5395432 | — | — | 1 | - |
| CHEMBL5429806 | — | — | 1 | - |
| CHEMBL5409581 | — | — | 1 | - |
| CHEMBL5399055 | — | — | 1 | - |
| CHEMBL5413817 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL280822 | CGP-20712A | Kd | = | 1.023 | nM | 8.99 |
| CHEMBL1326499 | — | Kd | = | 37.15 | nM | 7.43 |
| CHEMBL5427527 | — | Kd | = | 102.33 | nM | 6.99 |
| CHEMBL513389 | ZENIDOLOL | Kd | = | 120.23 | nM | 6.92 |
| CHEMBL5397120 | — | Kd | = | 134.9 | nM | 6.87 |
| CHEMBL5430355 | — | Kd | = | 257.04 | nM | 6.59 |
| CHEMBL4238084 | — | Kd | = | 338.84 | nM | 6.47 |
| CHEMBL5415148 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL5428413 | — | Kd | = | 1659.59 | nM | 5.78 |
| CHEMBL5416996 | — | Kd | = | 1737.8 | nM | 5.76 |
| CHEMBL5431834 | — | Kd | = | 2290.87 | nM | 5.64 |
| CHEMBL5422259 | — | Kd | = | 2398.83 | nM | 5.62 |
| CHEMBL5395772 | — | Kd | = | 3090.3 | nM | 5.51 |
| CHEMBL5432691 | — | Kd | = | 3162.28 | nM | 5.50 |
| CHEMBL5437540 | — | Kd | = | 3235.94 | nM | 5.49 |
| CHEMBL5423415 | — | Kd | = | 3630.78 | nM | 5.44 |
| CHEMBL5432967 | — | Kd | = | 3630.78 | nM | 5.44 |
| CHEMBL5426087 | — | Kd | = | 3890.45 | nM | 5.41 |
| CHEMBL5430136 | — | Kd | = | 5623.41 | nM | 5.25 |
| CHEMBL5402516 | — | Kd | = | 6025.6 | nM | 5.22 |
| CHEMBL5434276 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5395675 | — | Kd | < | 0.1 | nM | - |
| CHEMBL5416424 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5413563 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5403431 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5395432 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5429806 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5409581 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5399055 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5413817 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5400977 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5417897 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5422894 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5410388 | — | Kd | > | 10000.0 | nM | - |