Assay Detail
Binding
CHEMBL1909214
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DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.26 | 6.60 |
| Ki | 871 | 5.52 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | 4.0 | 2 | 6.85 |
| CHEMBL115769 | — | — | 2 | 6.24 |
| CHEMBL290106 | BITHIONOL | 4.0 | 2 | 6.18 |
| CHEMBL1475 | TRIOXSALEN | 4.0 | 2 | 6.13 |
| CHEMBL42442 | OXFENDAZOLE | 2.0 | 2 | 6.07 |
| CHEMBL496 | HEXACHLOROPHENE | 4.0 | 2 | 6.04 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 5.93 |
| CHEMBL64894 | GENTIAN VIOLET | 4.0 | 2 | 5.72 |
| CHEMBL1726 | NISOLDIPINE | 4.0 | 2 | 5.64 |
| CHEMBL1282 | IMIQUIMOD | 4.0 | 2 | 5.53 |
| CHEMBL10 | SB-203580 | — | 2 | 5.47 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 2 | 5.40 |
| CHEMBL9514 | NOCODAZOLE | 2.0 | 2 | 5.38 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 2 | 5.30 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 2 | 5.17 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 2 | 5.15 |
| CHEMBL91 | MICONAZOLE | 4.0 | 2 | 5.10 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 5.09 |
| CHEMBL44 | GENISTEIN | 2.0 | 2 | 5.01 |
| CHEMBL113 | CAFFEINE | 4.0 | 2 | 4.94 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 2 | 4.93 |
| CHEMBL195437 | 4-OCTYLPHENOL | — | 2 | 4.90 |
| CHEMBL434063 | — | — | 2 | 4.68 |
| CHEMBL1095699 | AZASERINE | 2.0 | 2 | - |
| CHEMBL701 | BACLOFEN | 4.0 | 2 | - |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | - |
| CHEMBL12089 | BERBERINE CHLORIDE | 1.0 | 2 | - |
| CHEMBL1231530 | BETAMIPRON | 2.0 | 2 | - |
| CHEMBL1077 | BROMFENAC | 4.0 | 2 | - |
| CHEMBL894 | BUPROPION | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL115769 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL290106 | BITHIONOL | Ki | = | 655.0 | nM | 6.18 |
| CHEMBL1475 | TRIOXSALEN | Ki | = | 737.0 | nM | 6.13 |
| CHEMBL42442 | OXFENDAZOLE | Ki | = | 844.0 | nM | 6.07 |
| CHEMBL496 | HEXACHLOROPHENE | Ki | = | 906.0 | nM | 6.04 |
| CHEMBL115769 | — | IC50 | = | 1032.0 | nM | 5.99 |
| CHEMBL290106 | BITHIONOL | IC50 | = | 1167.0 | nM | 5.93 |
| CHEMBL81 | RALOXIFENE | Ki | = | 1185.0 | nM | 5.93 |
| CHEMBL1475 | TRIOXSALEN | IC50 | = | 1312.0 | nM | 5.88 |
| CHEMBL42442 | OXFENDAZOLE | IC50 | = | 1504.0 | nM | 5.82 |
| CHEMBL496 | HEXACHLOROPHENE | IC50 | = | 1613.8 | nM | 5.79 |
| CHEMBL64894 | GENTIAN VIOLET | Ki | = | 1889.0 | nM | 5.72 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 2111.0 | nM | 5.68 |
| CHEMBL1726 | NISOLDIPINE | Ki | = | 2278.0 | nM | 5.64 |
| CHEMBL1282 | IMIQUIMOD | Ki | = | 2987.0 | nM | 5.53 |
| CHEMBL64894 | GENTIAN VIOLET | IC50 | = | 3365.0 | nM | 5.47 |
| CHEMBL10 | SB-203580 | Ki | = | 3407.0 | nM | 5.47 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 3985.0 | nM | 5.40 |
| CHEMBL1726 | NISOLDIPINE | IC50 | = | 4058.0 | nM | 5.39 |
| CHEMBL9514 | NOCODAZOLE | Ki | = | 4219.0 | nM | 5.38 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 5060.0 | nM | 5.30 |
| CHEMBL1282 | IMIQUIMOD | IC50 | = | 5320.0 | nM | 5.27 |
| CHEMBL10 | SB-203580 | IC50 | = | 6068.0 | nM | 5.22 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6741.0 | nM | 5.17 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 7099.0 | nM | 5.15 |
| CHEMBL104 | CLOTRIMAZOLE | Ki | = | 7136.0 | nM | 5.15 |
| CHEMBL9514 | NOCODAZOLE | IC50 | = | 7509.0 | nM | 5.12 |
| CHEMBL91 | MICONAZOLE | Ki | = | 8002.0 | nM | 5.10 |
| CHEMBL808 | ECONAZOLE | Ki | = | 8206.0 | nM | 5.09 |
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | = | 9013.0 | nM | 5.04 |
| CHEMBL44 | GENISTEIN | Ki | = | 9792.0 | nM | 5.01 |
| CHEMBL113 | CAFFEINE | Ki | = | 11493.0 | nM | 4.94 |
| CHEMBL691 | ETHINYL ESTRADIOL | Ki | = | 11751.0 | nM | 4.93 |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | = | 12007.0 | nM | 4.92 |
| CHEMBL195437 | 4-OCTYLPHENOL | Ki | = | 12593.0 | nM | 4.90 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 12711.0 | nM | 4.90 |
| CHEMBL91 | MICONAZOLE | IC50 | = | 14253.0 | nM | 4.85 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 14616.0 | nM | 4.83 |
| CHEMBL44 | GENISTEIN | IC50 | = | 17442.0 | nM | 4.76 |
| CHEMBL113 | CAFFEINE | IC50 | = | 20472.0 | nM | 4.69 |
| CHEMBL691 | ETHINYL ESTRADIOL | IC50 | = | 20931.0 | nM | 4.68 |
| CHEMBL434063 | — | Ki | = | 20915.0 | nM | 4.68 |
| CHEMBL195437 | 4-OCTYLPHENOL | IC50 | = | 22432.0 | nM | 4.65 |
| CHEMBL434063 | — | IC50 | = | 37254.0 | nM | 4.43 |
| CHEMBL1909071 | — | IC50 | - | — | - | |
| CHEMBL286398 | PROPYLENE GLYCOL | IC50 | - | — | - | |
| CHEMBL286398 | PROPYLENE GLYCOL | Ki | - | — | - | |
| CHEMBL1221512 | — | IC50 | - | — | - |