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Assay Detail

CHEMBL642845

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory activity against acyl-CoA:cholesterol O-acyltransferase (ACAT)
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sterol O-acyltransferase 1 (CHEMBL285)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)
Obata R, Sunazuka T, Tomoda H, Harigaya Y, Omura S
Bioorg Med Chem Lett (1995) 5 : 2683 -2688
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.17 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330686 1 8.22
CHEMBL91931 1 7.89
CHEMBL327774 1 7.72
CHEMBL90822 1 7.60
CHEMBL88379 1 7.48
CHEMBL89227 1 7.42
CHEMBL328676 1 7.41
CHEMBL89348 1 7.17
CHEMBL310661 1 7.07
CHEMBL88907 1 7.07
CHEMBL25532 1 7.05
CHEMBL329588 1 6.92
CHEMBL422065 1 6.89
CHEMBL421887 1 6.89
CHEMBL89197 1 6.85
CHEMBL91822 1 6.70
CHEMBL91466 1 6.57
CHEMBL314631 1 6.21
CHEMBL432037 1 6.04
CHEMBL327483 1 5.92
CHEMBL91530 1 5.75
CHEMBL90228 1 5.68
CHEMBL441168 1 5.68
CHEMBL328021 1 5.62
CHEMBL315952 1 5.60
CHEMBL91725 1 5.51
CHEMBL330051 1 5.38
CHEMBL91606 1 5.29
CHEMBL89160 1 5.24
CHEMBL88457 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330686 IC50 = 6.0 nM 8.22
CHEMBL91931 IC50 = 13.0 nM 7.89
CHEMBL327774 IC50 = 19.0 nM 7.72
CHEMBL90822 IC50 = 25.0 nM 7.60
CHEMBL88379 IC50 = 33.0 nM 7.48
CHEMBL89227 IC50 = 38.0 nM 7.42
CHEMBL328676 IC50 = 39.0 nM 7.41
CHEMBL89348 IC50 = 67.0 nM 7.17
CHEMBL310661 IC50 = 85.0 nM 7.07
CHEMBL88907 IC50 = 86.0 nM 7.07
CHEMBL25532 IC50 = 89.0 nM 7.05
CHEMBL329588 IC50 = 120.0 nM 6.92
CHEMBL422065 IC50 = 130.0 nM 6.89
CHEMBL421887 IC50 = 130.0 nM 6.89
CHEMBL89197 IC50 = 140.0 nM 6.85
CHEMBL91822 IC50 = 200.0 nM 6.70
CHEMBL91466 IC50 = 270.0 nM 6.57
CHEMBL314631 IC50 = 620.0 nM 6.21
CHEMBL432037 IC50 = 910.0 nM 6.04
CHEMBL327483 IC50 = 1200.0 nM 5.92
CHEMBL91530 IC50 = 1800.0 nM 5.75
CHEMBL90228 IC50 = 2100.0 nM 5.68
CHEMBL441168 IC50 = 2100.0 nM 5.68
CHEMBL328021 IC50 = 2400.0 nM 5.62
CHEMBL315952 IC50 = 2500.0 nM 5.60
CHEMBL91725 IC50 = 3100.0 nM 5.51
CHEMBL330051 IC50 = 4200.0 nM 5.38
CHEMBL91606 IC50 = 5100.0 nM 5.29
CHEMBL89160 IC50 = 5800.0 nM 5.24
CHEMBL88457 IC50 = 5800.0 nM 5.24
CHEMBL328559 IC50 = 5900.0 nM 5.23
CHEMBL315860 IC50 = 7400.0 nM 5.13
CHEMBL311537 IC50 = 16000.0 nM 4.80
CHEMBL330039 IC50 = 23000.0 nM 4.64
CHEMBL329587 IC50 = 38000.0 nM 4.42
CHEMBL328544 IC50 = 79000.0 nM 4.10
CHEMBL91306 IC50 = 100000.0 nM 4.00
CHEMBL431209 IC50 > 8000.0 nM -
CHEMBL329767 IC50 > 180000.0 nM -
CHEMBL329584 IC50 = 110000.0 nM -
CHEMBL88875 IC50 > 200000.0 nM -
CHEMBL368221 IC50 > 220000.0 nM -