Assay Detail
Functional
CHEMBL781269
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [3H]GABA uptake in rat Hippocampal slices.
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 5.28 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2093906 | — | — | 2 | 6.75 |
| CHEMBL542207 | — | — | 1 | 6.47 |
| CHEMBL543672 | — | — | 1 | 6.39 |
| CHEMBL557404 | — | — | 1 | 6.39 |
| CHEMBL538041 | — | — | 1 | 6.16 |
| CHEMBL556406 | — | — | 1 | 6.15 |
| CHEMBL555322 | — | — | 1 | 6.04 |
| CHEMBL540323 | — | — | 1 | 5.96 |
| CHEMBL539619 | — | — | 1 | 5.92 |
| CHEMBL543198 | — | — | 1 | 5.92 |
| CHEMBL538037 | — | — | 1 | 5.85 |
| CHEMBL555769 | — | — | 1 | 5.82 |
| CHEMBL554464 | — | — | 1 | 5.80 |
| CHEMBL544841 | — | — | 1 | 5.60 |
| CHEMBL71789 | — | — | 1 | 5.60 |
| CHEMBL135003 | — | — | 1 | 5.57 |
| CHEMBL76966 | — | — | 1 | 5.51 |
| CHEMBL553153 | — | — | 1 | 5.50 |
| CHEMBL542610 | — | — | 1 | 5.47 |
| CHEMBL335266 | — | — | 1 | 5.44 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.28 |
| CHEMBL544612 | — | — | 1 | 5.24 |
| CHEMBL76768 | GUVACINE | — | 1 | 5.14 |
| CHEMBL559193 | — | — | 1 | 5.11 |
| CHEMBL422277 | — | — | 1 | 5.10 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.07 |
| CHEMBL134637 | — | — | 1 | 5.06 |
| CHEMBL38686 | — | — | 1 | 5.00 |
| CHEMBL542961 | — | — | 1 | 4.96 |
| CHEMBL132437 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2093906 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL542207 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL557404 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL543672 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL538041 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL556406 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL555322 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL540323 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL539619 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL543198 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL538037 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL555769 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL554464 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL71789 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL544841 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL135003 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL76966 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL553153 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL542610 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL335266 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL544612 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL76768 | GUVACINE | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL559193 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL422277 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL134637 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL38686 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL542961 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL132437 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2093906 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL539555 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL541849 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL542962 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL558416 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL538780 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL135980 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL539038 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL540062 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL134621 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL558380 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL555779 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL555092 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL108 | CARBAMAZEPINE | IC50 | > | 50000.0 | nM | - |
| CHEMBL552604 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL135575 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL109 | VALPROIC ACID | IC50 | > | 50000.0 | nM | - |
| CHEMBL554948 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL542735 | — | IC50 | > | 50000.0 | nM | - |