Assay Detail
Binding
CHEMBL3887218
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Scintillation Proximity Assay (SPA) Assay: SPA membrane binding assay was used to identify inhibitors of [33P] 2MeS-ADP binding to cloned human P2Yi receptors (The P2Yi receptor membranes were provided by Biology and the cloning of the receptor and P2Yi receptor membrane preparation is same as described by Biology). Binding reactions were performed in 384- well OptiPlates (PerkinElmer Life Sciences, Cat # 6007299) in a volume of 50 ui containing -15 fmol of P2Y1 receptor (1.7 ug of total protein), 0.3 nM [33P] 2MeS-ADP(PerkinElmer; 2,000 Ci/mmol), various concentrations of the test compound (usually between 10 uM and 160 pM) in Buffer B containing 1% DMSO in assay buffer (15 mM, HEPES, 145 mM potassium chloride, 5 mM sodium Chloride, 5 mM EDTA, 0.1 mM MgCl2, pH 7.4) and 100 ug of SPA bead (WGA polystyrene Image beads, #RPNQ 0260V, Amersham). Reactions were allowed to proceed to completion at room temperature for 1 hour followed by centrifugation of the plate for 5 min.
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Amino-heteroaryl 7-hydroxy-spiropiperidine indolinyl antagonists of P2Y1 receptor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.77 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3920135 | — | — | 1 | 8.52 |
| CHEMBL3263070 | — | — | 1 | 8.30 |
| CHEMBL3263058 | — | — | 1 | 8.22 |
| CHEMBL3903953 | — | — | 1 | 8.22 |
| CHEMBL3932713 | — | — | 1 | 8.17 |
| CHEMBL3896467 | — | — | 1 | 8.15 |
| CHEMBL3967844 | — | — | 1 | 8.10 |
| CHEMBL3263069 | — | — | 1 | 8.10 |
| CHEMBL3926419 | — | — | 1 | 8.10 |
| CHEMBL3973199 | — | — | 1 | 8.05 |
| CHEMBL3263068 | — | — | 1 | 8.00 |
| CHEMBL3263057 | — | — | 1 | 8.00 |
| CHEMBL3900332 | — | — | 1 | 7.96 |
| CHEMBL3928274 | — | — | 1 | 7.92 |
| CHEMBL3263071 | — | — | 1 | 7.89 |
| CHEMBL3263074 | — | — | 1 | 7.89 |
| CHEMBL3893716 | — | — | 1 | 7.82 |
| CHEMBL3263073 | — | — | 1 | 7.80 |
| CHEMBL3263066 | — | — | 1 | 7.80 |
| CHEMBL3263062 | — | — | 1 | 7.80 |
| CHEMBL3927367 | — | — | 1 | 7.72 |
| CHEMBL3905619 | — | — | 1 | 7.72 |
| CHEMBL3918409 | — | — | 1 | 7.72 |
| CHEMBL3981201 | — | — | 1 | 7.68 |
| CHEMBL3911187 | — | — | 1 | 7.66 |
| CHEMBL3929983 | — | — | 1 | 7.66 |
| CHEMBL3979693 | — | — | 1 | 7.64 |
| CHEMBL3893862 | — | — | 1 | 7.64 |
| CHEMBL3890364 | — | — | 1 | 7.62 |
| CHEMBL3263067 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3920135 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3263070 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3263058 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3903953 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3932713 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3896467 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3967844 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3263069 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3926419 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3973199 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3263057 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3263068 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3900332 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3928274 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3263074 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3263071 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3893716 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3263073 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3263066 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3263062 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3927367 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3918409 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3905619 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3981201 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3911187 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3929983 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3979693 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3893862 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3890364 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3263067 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3263072 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3902900 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3898478 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3968470 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3956460 | — | IC50 | = | 40.2 | nM | 7.40 |
| CHEMBL3901946 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3932841 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3263060 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3972991 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3974841 | — | IC50 | = | 69.0 | nM | 7.16 |