Assay Detail
Binding
CHEMBL5739367
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Metabolic Measurements: Glucose in tail blood was measured using a glucometer (One-Touch Basic; Lifescan, CA). For glucose tolerance tests (GTTs), mice were fasted for 10 hours and then injected with 20% D-glucose (2 mg/g body weight) and the blood glucose was monitored immediately before and at 15, 30, 60 and 120 mins following the injection. For insulin tolerance tests (ITTs), 4-h fasted animals were given insulin (0.75 mU/g) and blood glucose was measured immediately before and at 30, 60 and 120 minutes postinjection. Serum insulin, cholesterol, triglycerides (Stanbio Labs, TX), BDNF (Abnova), IGF1 and IGFBPs (R&D Systems) were determined by enzyme-linked immunosorbent assay.
84
Total Activities
28
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Treatment of Rett syndrome
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.35 | 6.16 |
| kon | 28 | - | - |
| k_off | 28 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6021058 | — | — | 3 | 6.16 |
| CHEMBL169 | URSOLIC ACID | 2.0 | 3 | 6.05 |
| CHEMBL399873 | UVAOL | — | 3 | 6.00 |
| CHEMBL289191 | LUPEOL | — | 3 | 5.82 |
| CHEMBL391533 | COROSOLIC ACID | — | 3 | 5.82 |
| CHEMBL5959887 | — | — | 3 | 5.70 |
| CHEMBL486400 | HEDERAGENIN | — | 3 | 5.70 |
| CHEMBL23236 | BETULIN | — | 3 | 5.70 |
| CHEMBL168 | OLEANOLIC_ACID | — | 3 | 5.70 |
| CHEMBL455357 | — | — | 3 | 5.40 |
| CHEMBL395428 | — | — | 3 | 5.40 |
| CHEMBL404519 | BEVIRIMAT | 2.0 | 3 | 5.36 |
| CHEMBL499915 | CARBENOXOLONE | 2.0 | 3 | 5.30 |
| CHEMBL472646 | MORONIC ACID | — | 3 | 5.30 |
| CHEMBL5792205 | — | — | 3 | 5.30 |
| CHEMBL5788057 | — | — | 3 | 5.24 |
| CHEMBL5811482 | — | — | 3 | 5.24 |
| CHEMBL5936573 | — | — | 3 | 5.22 |
| CHEMBL464466 | ARJUNOLIC ACID | — | 3 | 5.16 |
| CHEMBL54804 | PRISTIMERIN | — | 3 | 5.10 |
| CHEMBL5802984 | — | — | 3 | 5.05 |
| CHEMBL3391893 | — | — | 3 | 5.00 |
| CHEMBL301982 | CELASTROL | — | 3 | 5.00 |
| CHEMBL230006 | ENOXOLONE | 2.0 | 3 | 5.00 |
| CHEMBL5997211 | — | — | 3 | 4.96 |
| CHEMBL5816719 | — | — | 3 | 4.82 |
| CHEMBL5907138 | — | — | 3 | 4.66 |
| CHEMBL400807 | — | — | 3 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6021058 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL169 | URSOLIC ACID | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL399873 | UVAOL | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL289191 | LUPEOL | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL391533 | COROSOLIC ACID | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL486400 | HEDERAGENIN | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL168 | OLEANOLIC_ACID | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL23236 | BETULIN | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL5959887 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL455357 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL395428 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL404519 | BEVIRIMAT | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL499915 | CARBENOXOLONE | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL5792205 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL472646 | MORONIC ACID | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL5788057 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL5811482 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL5936573 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL464466 | ARJUNOLIC ACID | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL54804 | PRISTIMERIN | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL5802984 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL3391893 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL301982 | CELASTROL | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL230006 | ENOXOLONE | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL5997211 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL5816719 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL5907138 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL400807 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL5802984 | — | k_off | = | - | s-1 | - |
| CHEMBL499915 | CARBENOXOLONE | kon | = | - | — | - |
| CHEMBL5811482 | — | k_off | = | - | s-1 | - |
| CHEMBL5811482 | — | kon | = | - | — | - |
| CHEMBL499915 | CARBENOXOLONE | k_off | = | - | s-1 | - |
| CHEMBL3391893 | — | kon | = | - | — | - |
| CHEMBL404519 | BEVIRIMAT | k_off | = | - | s-1 | - |
| CHEMBL3391893 | — | k_off | = | - | s-1 | - |
| CHEMBL404519 | BEVIRIMAT | kon | = | - | — | - |
| CHEMBL5792205 | — | kon | = | - | — | - |
| CHEMBL5792205 | — | k_off | = | - | s-1 | - |
| CHEMBL5802984 | — | kon | = | - | — | - |
| CHEMBL455357 | — | kon | = | - | — | - |
| CHEMBL5907138 | — | kon | = | - | — | - |
| CHEMBL472646 | MORONIC ACID | k_off | = | - | s-1 | - |
| CHEMBL5907138 | — | k_off | = | - | s-1 | - |
| CHEMBL472646 | MORONIC ACID | kon | = | - | — | - |
| CHEMBL400807 | — | kon | = | - | — | - |
| CHEMBL5997211 | — | k_off | = | - | s-1 | - |
| CHEMBL5997211 | — | kon | = | - | — | - |
| CHEMBL400807 | — | k_off | = | - | s-1 | - |
| CHEMBL455357 | — | k_off | = | - | s-1 | - |