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Assay Detail

CHEMBL4258459

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

Binding
Inhibition of porcine CEase using para-nitrophenyl butyrate as substrate preincubated with substrate for 5 mins followed by enzyme addition by spectrophotometric method
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

5,6-Benzoflavones as cholesterol esterase inhibitors: synthesis, biological evaluation and docking studies.
Singh JV, Kaur A, Bhagat K, Gupta MK, Singh M, Singh H, Bedi PMS.
Medchemcomm (2018) 9 : 490 -502
PubMed 30108939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.22 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285597 1 9.14
CHEMBL4277189 1 9.14
CHEMBL4292778 1 9.08
CHEMBL4278699 1 9.00
CHEMBL4289364 1 8.97
CHEMBL4282167 1 8.94
CHEMBL600169 1 8.92
CHEMBL4283803 1 8.84
CHEMBL599338 1 8.59
CHEMBL4284177 1 8.41
CHEMBL4292058 1 8.35
CHEMBL4277659 1 8.33
CHEMBL4288983 1 8.22
CHEMBL4284553 1 8.09
CHEMBL4292384 1 8.02
CHEMBL4281483 1 8.01
CHEMBL4284491 1 7.88
CHEMBL4278030 1 7.78
CHEMBL4285956 1 7.74
CHEMBL4284062 1 7.70
CHEMBL4294040 1 7.65
CHEMBL4281076 1 7.64
CHEMBL4290837 1 7.56
CHEMBL4280204 1 7.54
CHEMBL4276771 1 7.54
CHEMBL4288299 1 7.50
CHEMBL26260 BETA-NAPHTHOFLAVONE 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285597 IC50 = 0.73 nM 9.14
CHEMBL4277189 IC50 = 0.72 nM 9.14
CHEMBL4292778 IC50 = 0.83 nM 9.08
CHEMBL4278699 IC50 = 0.99 nM 9.00
CHEMBL4289364 IC50 = 1.08 nM 8.97
CHEMBL4282167 IC50 = 1.15 nM 8.94
CHEMBL600169 IC50 = 1.19 nM 8.92
CHEMBL4283803 IC50 = 1.46 nM 8.84
CHEMBL599338 IC50 = 2.59 nM 8.59
CHEMBL4284177 IC50 = 3.9 nM 8.41
CHEMBL4292058 IC50 = 4.5 nM 8.35
CHEMBL4277659 IC50 = 4.69 nM 8.33
CHEMBL4288983 IC50 = 6.01 nM 8.22
CHEMBL4284553 IC50 = 8.15 nM 8.09
CHEMBL4292384 IC50 = 9.55 nM 8.02
CHEMBL4281483 IC50 = 9.8 nM 8.01
CHEMBL4284491 IC50 = 13.11 nM 7.88
CHEMBL4278030 IC50 = 16.44 nM 7.78
CHEMBL4285956 IC50 = 18.01 nM 7.74
CHEMBL4284062 IC50 = 20.05 nM 7.70
CHEMBL4294040 IC50 = 22.23 nM 7.65
CHEMBL4281076 IC50 = 23.11 nM 7.64
CHEMBL4290837 IC50 = 27.79 nM 7.56
CHEMBL4280204 IC50 = 29.17 nM 7.54
CHEMBL4276771 IC50 = 29.11 nM 7.54
CHEMBL4288299 IC50 = 31.35 nM 7.50
CHEMBL26260 BETA-NAPHTHOFLAVONE IC50 = 51.06 nM 7.29