Assay Detail
Binding
CHEMBL915381
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Activity at human alpha-1-beta-GlyR expressed in HEK293 cells by FMP assay
45
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 5.56 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113267 | GINKGOLIDE M | — | 2 | 6.30 |
| CHEMBL465161 | GINKGOLIDE A | — | 2 | 6.20 |
| CHEMBL514432 | GINKOLIDE B | — | 2 | 5.70 |
| CHEMBL221821 | GINKGOLIDE C | — | 2 | 5.62 |
| CHEMBL373969 | 3,14-DIDEHYDROGINKGOLIDE A | — | 2 | 5.51 |
| CHEMBL221715 | — | — | 2 | 5.50 |
| CHEMBL426556 | — | — | 2 | 5.50 |
| CHEMBL374004 | GINKGOLIDE J | — | 2 | 5.40 |
| CHEMBL221823 | — | — | 2 | 5.30 |
| CHEMBL376289 | — | — | 2 | 5.13 |
| CHEMBL388075 | — | — | 2 | 5.10 |
| CHEMBL373832 | — | — | 1 | - |
| CHEMBL375821 | — | — | 1 | - |
| CHEMBL374058 | — | — | 1 | - |
| CHEMBL222345 | — | — | 1 | - |
| CHEMBL223761 | — | — | 1 | - |
| CHEMBL224937 | — | — | 1 | - |
| CHEMBL376777 | — | — | 1 | - |
| CHEMBL225471 | — | — | 1 | - |
| CHEMBL221355 | — | — | 1 | - |
| CHEMBL222405 | — | — | 1 | - |
| CHEMBL221937 | — | — | 1 | - |
| CHEMBL221769 | — | — | 1 | - |
| CHEMBL374102 | — | — | 1 | - |
| CHEMBL223081 | — | — | 1 | - |
| CHEMBL412540 | — | — | 1 | - |
| CHEMBL225470 | 10-METHOXYMETHYLOXY-GINKGOLIDE A | — | 1 | - |
| CHEMBL412384 | — | — | 1 | - |
| CHEMBL222222 | 10-ACETOXY-GINKGOLIDE B | — | 1 | - |
| CHEMBL376302 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113267 | GINKGOLIDE M | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2113267 | GINKGOLIDE M | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL465161 | GINKGOLIDE A | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL465161 | GINKGOLIDE A | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL514432 | GINKOLIDE B | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL514432 | GINKOLIDE B | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL221821 | GINKGOLIDE C | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL221821 | GINKGOLIDE C | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL373969 | 3,14-DIDEHYDROGINKGOLIDE A | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL221715 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL221715 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL426556 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL426556 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL373969 | 3,14-DIDEHYDROGINKGOLIDE A | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL374004 | GINKGOLIDE J | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL374004 | GINKGOLIDE J | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL221823 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL221823 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL376289 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL388075 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL376289 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL388075 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL373436 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL385320 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL222534 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL387106 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL373832 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL375821 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL374058 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL222345 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL223761 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL224937 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL376777 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL225471 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL222222 | 10-ACETOXY-GINKGOLIDE B | IC50 | > | 100000.0 | nM | - |
| CHEMBL412384 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL225470 | 10-METHOXYMETHYLOXY-GINKGOLIDE A | IC50 | > | 100000.0 | nM | - |
| CHEMBL412540 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL223081 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL374102 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL221769 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL221937 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL222405 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL376302 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL221355 | — | IC50 | > | 100000.0 | nM | - |