Assay Detail
Binding
CHEMBL3705647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The stable cell line expressing human SGLT1 was seeded at 5x104 cells/well on BioCoat Poly-D-Lysine 96 well plate with Lid (Becton Dickinson and Company) and cultured at 37 C. under 5% CO2 overnight. The medium was replaced with 100 uL/well of a Na (+) buffer (140 mM choline chloride, 2 mM KCl, 1 mM MgCl2, 1 mM CaCl2, 10 mM HEPES, 5 mM Tris, pH7.4) followed by incubation for 20 minutes at 37 C. under 5% CO2. After removing the Na (+) buffer, a test compound solution which was prepared from Na (+) buffer (140 mM NaCl, 2 mM KCl, 1 mM MgCl2, 1 mM CaCl2, 10 mM HEPES, 5 mM Tris, pH7.4) containing BSA was added thereto at 40 uL/well. In addition, Na (+) buffer containing 8 kBq of 14C-AMG and 2 mM AMG was added thereto at 40 uL/well, and was mixed well. Na (+) buffer containing BSA was added to a blank well at 40 uL/well and additionally adding a Na (+) buffer containing 8 kBq of 14C-AMG and 2 mM AMG, and was mixed well.
520
Total Activities
511
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrazole compound and pharmaceutical use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 520 | 7.84 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3690855 | — | — | 1 | 9.15 |
| CHEMBL3686477 | — | — | 1 | 9.05 |
| CHEMBL3686485 | — | — | 1 | 8.96 |
| CHEMBL3690821 | — | — | 1 | 8.96 |
| CHEMBL3695107 | — | — | 1 | 8.96 |
| CHEMBL3686471 | — | — | 1 | 8.92 |
| CHEMBL3686475 | — | — | 1 | 8.89 |
| CHEMBL3686489 | — | — | 1 | 8.89 |
| CHEMBL3690854 | — | — | 1 | 8.89 |
| CHEMBL3690868 | — | — | 1 | 8.89 |
| CHEMBL3695108 | — | — | 1 | 8.85 |
| CHEMBL3695105 | — | — | 1 | 8.85 |
| CHEMBL3690875 | — | — | 1 | 8.85 |
| CHEMBL3686472 | — | — | 1 | 8.85 |
| CHEMBL3686463 | — | — | 1 | 8.85 |
| CHEMBL3690863 | — | — | 1 | 8.85 |
| CHEMBL3686483 | — | — | 1 | 8.82 |
| CHEMBL3690942 | — | — | 1 | 8.82 |
| CHEMBL3690989 | — | — | 1 | 8.82 |
| CHEMBL3686422 | — | — | 1 | 8.80 |
| CHEMBL3686484 | — | — | 1 | 8.77 |
| CHEMBL3695109 | — | — | 1 | 8.77 |
| CHEMBL3695097 | — | — | 1 | 8.77 |
| CHEMBL3695096 | — | — | 1 | 8.77 |
| CHEMBL3686428 | — | — | 1 | 8.77 |
| CHEMBL3686379 | — | — | 1 | 8.74 |
| CHEMBL3686440 | — | — | 1 | 8.74 |
| CHEMBL3695170 | — | — | 1 | 8.74 |
| CHEMBL3686447 | — | — | 1 | 8.72 |
| CHEMBL3686429 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3690855 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3686477 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3695107 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3686485 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3690821 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3686471 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3690868 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3686475 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3690854 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3686489 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3686472 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3695105 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3695108 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3690863 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3686463 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3690875 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3686483 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3690942 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3690989 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3686422 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3695109 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3695097 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3695096 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3686428 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3686484 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3695170 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3686440 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3686379 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3686447 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3695098 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3686429 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3695079 | — | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL3695169 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3690883 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3695104 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3695161 | — | IC50 | = | 2.15 | nM | 8.67 |
| CHEMBL3686449 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3690960 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3690874 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3695167 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3695093 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3690879 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3695072 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL3686443 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3686448 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3690831 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3690978 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3690823 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3695171 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3690833 | — | IC50 | = | 2.9 | nM | 8.54 |