Assay Detail
Functional
CHEMBL964514
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
32
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit rho-1 (CHEMBL3561) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kb | 26 | - | - |
| IC50 | 6 | 4.79 | 5.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL109375 | — | — | 1 | 5.26 |
| CHEMBL601 | AMINOLEVULINIC ACID | 4.0 | 1 | 4.89 |
| CHEMBL112797 | SGS-742 | 2.0 | 1 | 4.21 |
| CHEMBL447036 | — | — | 2 | - |
| CHEMBL451118 | — | — | 2 | - |
| CHEMBL487279 | — | — | 1 | - |
| CHEMBL446306 | — | — | 1 | - |
| CHEMBL486434 | — | — | 1 | - |
| CHEMBL507241 | — | — | 1 | - |
| CHEMBL507116 | — | — | 1 | - |
| CHEMBL453966 | — | — | 1 | - |
| CHEMBL447171 | — | — | 1 | - |
| CHEMBL445449 | — | — | 1 | - |
| CHEMBL504482 | — | — | 1 | - |
| CHEMBL355921 | — | — | 2 | - |
| CHEMBL41905 | — | — | 1 | - |
| CHEMBL397209 | — | — | 1 | - |
| CHEMBL453505 | — | — | 1 | - |
| CHEMBL460473 | — | — | 1 | - |
| CHEMBL500625 | — | — | 1 | - |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 1 | - |
| CHEMBL112710 | — | — | 1 | - |
| CHEMBL430510 | — | — | 1 | - |
| CHEMBL284115 | — | — | 1 | - |
| CHEMBL230115 | — | — | 1 | - |
| CHEMBL290961 | — | — | 1 | - |
| CHEMBL312443 | GABOXADOL | 3.0 | 1 | - |
| CHEMBL284116 | 5-AMINOVALERIC ACID | 1.0 | 1 | - |
| CHEMBL449512 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL109375 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL601 | AMINOLEVULINIC ACID | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL112797 | SGS-742 | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL447036 | — | Kb | > | 300000.0 | nM | - |
| CHEMBL447036 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL451118 | — | Kb | > | 300000.0 | nM | - |
| CHEMBL355921 | — | Kb | = | 6000.0 | nM | - |
| CHEMBL504482 | — | Kb | = | 1840.0 | nM | - |
| CHEMBL445449 | — | Kb | = | 18900.0 | nM | - |
| CHEMBL447171 | — | Kb | = | 780.0 | nM | - |
| CHEMBL453966 | — | Kb | = | 3530.0 | nM | - |
| CHEMBL507116 | — | Kb | = | 13100.0 | nM | - |
| CHEMBL507241 | — | Kb | = | 7240.0 | nM | - |
| CHEMBL486434 | — | Kb | = | 59300.0 | nM | - |
| CHEMBL446306 | — | Kb | = | 4970.0 | nM | - |
| CHEMBL487279 | — | Kb | = | 48600.0 | nM | - |
| CHEMBL451118 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL41905 | — | Kb | = | 6000.0 | nM | - |
| CHEMBL397209 | — | Kb | = | 2100.0 | nM | - |
| CHEMBL453505 | — | Kb | = | 1100.0 | nM | - |
| CHEMBL460473 | — | Kb | = | 6600.0 | nM | - |
| CHEMBL500625 | — | Kb | = | 1100.0 | nM | - |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | Kb | = | 1700.0 | nM | - |
| CHEMBL112710 | — | Kb | = | 800.0 | nM | - |
| CHEMBL430510 | — | Kb | = | 38900.0 | nM | - |
| CHEMBL284115 | — | Kb | = | 45000.0 | nM | - |
| CHEMBL230115 | — | IC50 | > | 800000.0 | nM | - |
| CHEMBL290961 | — | Kb | = | 950.0 | nM | - |
| CHEMBL312443 | GABOXADOL | Kb | = | 32000.0 | nM | - |
| CHEMBL284116 | 5-AMINOVALERIC ACID | Kb | = | 20000.0 | nM | - |
| CHEMBL355921 | — | Kb | = | 6100.0 | nM | - |
| CHEMBL449512 | — | Kb | = | 6600.0 | nM | - |