Assay Detail
Binding
CHEMBL3889231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cholesteryl Ester Transfer Assay: As a protein source for cholesteryl ester transfer, plasma from healthy persons was used, and as a cholesteryl ester receptor, LDL from healthy persons was used. Samples were treated with each test compound to final concentrations of 16, 80, 400, 2000 and 10000 nM and analyzed in duplicate. For the cholesteryl ester transfer test, 20 μl of plasma, 50 μl of LDL (0.25 mg/ml) and 50 μl of rHDL-agarose (0.25 mg/ml) were added, and a solution containing a test compound was added, followed by reaction at 37° C. Then, centrifugation was performed at 4° C. for 3 minutes to stop the reaction, and 150 μl of the supernatant was taken and transferred to a 96-well plate for radioactivity measurement, and the radioactivity of the plate was measured with a beta-ray detector.
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 8.04 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3906320 | — | — | 1 | 8.82 |
| CHEMBL3914103 | — | — | 1 | 8.80 |
| CHEMBL3965631 | — | — | 1 | 8.72 |
| CHEMBL3955558 | — | — | 1 | 8.72 |
| CHEMBL3982930 | — | — | 1 | 8.60 |
| CHEMBL3972983 | — | — | 1 | 8.41 |
| CHEMBL3953367 | — | — | 1 | 8.30 |
| CHEMBL3948773 | — | — | 1 | 8.28 |
| CHEMBL3986115 | — | — | 1 | 8.27 |
| CHEMBL3927226 | — | — | 1 | 8.24 |
| CHEMBL3898351 | — | — | 1 | 8.23 |
| CHEMBL3987174 | — | — | 1 | 8.19 |
| CHEMBL3941193 | — | — | 1 | 8.18 |
| CHEMBL3915159 | — | — | 1 | 8.16 |
| CHEMBL3926422 | — | — | 1 | 8.15 |
| CHEMBL3932190 | — | — | 1 | 8.14 |
| CHEMBL3912017 | — | — | 1 | 8.12 |
| CHEMBL3928848 | — | — | 1 | 8.12 |
| CHEMBL3949935 | — | — | 1 | 8.08 |
| CHEMBL3897170 | — | — | 1 | 8.05 |
| CHEMBL3891904 | — | — | 1 | 8.04 |
| CHEMBL3920961 | — | — | 1 | 8.02 |
| CHEMBL3926760 | — | — | 1 | 7.97 |
| CHEMBL3942098 | — | — | 1 | 7.94 |
| CHEMBL3919350 | — | — | 1 | 7.94 |
| CHEMBL3954404 | — | — | 1 | 7.92 |
| CHEMBL3897353 | — | — | 1 | 7.91 |
| CHEMBL3980987 | — | — | 1 | 7.90 |
| CHEMBL3978985 | — | — | 1 | 7.89 |
| CHEMBL3943442 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3906320 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3914103 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3955558 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3965631 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3982930 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3972983 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3953367 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3948773 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3986115 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3927226 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3898351 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3987174 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3941193 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3915159 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3926422 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3932190 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3912017 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL3928848 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3949935 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3897170 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3891904 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3920961 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL3926760 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL3942098 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL3919350 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL3954404 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL3897353 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL3980987 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL3978985 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3943442 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL3971977 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3970749 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL3907248 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL3934300 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL3910458 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL3957430 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL3924471 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL3919949 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3951447 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL3890674 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL3897306 | — | IC50 | = | 56.6 | nM | 7.25 |