Assay Detail
Binding
CHEMBL646539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of acyl coenzyme A:cholesterol acyltransferase, in intestinal microsomes isolated from cholesterol-fed rabbits
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Intestine |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Acyl-CoA:cholesterol acyltransferase (CHEMBL6141) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 67 | 6.61 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL40608 | — | — | 1 | 8.15 |
| CHEMBL42998 | — | — | 1 | 7.82 |
| CHEMBL417517 | — | — | 1 | 7.77 |
| CHEMBL289033 | — | — | 1 | 7.70 |
| CHEMBL40527 | — | — | 1 | 7.64 |
| CHEMBL44020 | — | — | 1 | 7.52 |
| CHEMBL41184 | — | — | 1 | 7.51 |
| CHEMBL442351 | — | — | 1 | 7.50 |
| CHEMBL41001 | — | — | 1 | 7.44 |
| CHEMBL42574 | — | — | 1 | 7.41 |
| CHEMBL43810 | — | — | 1 | 7.36 |
| CHEMBL40547 | — | — | 1 | 7.36 |
| CHEMBL38789 | — | — | 1 | 7.31 |
| CHEMBL41330 | — | — | 1 | 7.28 |
| CHEMBL295831 | — | — | 1 | 7.28 |
| CHEMBL40809 | — | — | 1 | 7.27 |
| CHEMBL417159 | — | — | 1 | 7.24 |
| CHEMBL40556 | — | — | 1 | 7.23 |
| CHEMBL42433 | — | — | 1 | 7.22 |
| CHEMBL295993 | — | — | 1 | 7.20 |
| CHEMBL44460 | — | — | 1 | 7.19 |
| CHEMBL297232 | — | — | 1 | 7.16 |
| CHEMBL22373 | CL-976 | — | 1 | 7.14 |
| CHEMBL41273 | — | — | 1 | 7.06 |
| CHEMBL41714 | — | — | 1 | 7.03 |
| CHEMBL42371 | — | — | 1 | 7.01 |
| CHEMBL290606 | — | — | 1 | 6.89 |
| CHEMBL40985 | — | — | 1 | 6.89 |
| CHEMBL288422 | — | — | 1 | 6.85 |
| CHEMBL42143 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL40608 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL42998 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL417517 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL289033 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL40527 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL44020 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL41184 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL442351 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL41001 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL42574 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL43810 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL40547 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL38789 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL295831 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL41330 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL40809 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL417159 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL40556 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL42433 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL295993 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL44460 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL297232 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL22373 | CL-976 | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL41273 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL41714 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL42371 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL40985 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL290606 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL288422 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL42143 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL294929 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL287932 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL41571 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL295156 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL44099 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL44016 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL289062 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL42732 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL298330 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL41085 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL40470 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL297834 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL40781 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL291164 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL42147 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL41891 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL41554 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL442157 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL43984 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL38836 | — | IC50 | = | 910.0 | nM | 6.04 |