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Assay Detail

CHEMBL4688056

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

Binding
Inhibition of porcine pancreatic lipase preincubated for 10 mins followed by 4-MUO addition and measured at 60 sec interval for 40 mins by multi plate micro plate reader
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Pancreatic triacylglycerol lipase (CHEMBL1687677)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Design, synthesis and biological evaluation of novel chalcone-like compounds as potent and reversible pancreatic lipase inhibitors.
Huo PC,Hu Q,Shu S,Zhou QH,He RJ,Hou J,Guan XQ,Tu DZ,Hou XD,Liu P,Zhang N,Liu ZG,Ge GB
Bioorg Med Chem (2021) 29 : 115853 -115853
PubMed 33214035 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.16 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365190 1 8.33
CHEMBL4780197 1 6.48
CHEMBL4788400 1 6.24
CHEMBL4797179 1 6.17
CHEMBL4782276 1 6.08
CHEMBL4748399 1 5.77
CHEMBL4757866 1 5.68
CHEMBL4744746 1 5.60
CHEMBL4752404 1 5.59
CHEMBL4740149 1 5.48
CHEMBL4776624 1 5.46
CHEMBL4761197 1 5.16
CHEMBL4745825 1 5.07
CHEMBL4747287 1 4.98
CHEMBL4751728 1 4.91
CHEMBL4160838 1 4.83
CHEMBL4778007 1 4.83
CHEMBL4080900 1 4.83
CHEMBL4780689 1 4.68
CHEMBL4765140 1 4.61
CHEMBL4750178 1 4.60
CHEMBL4098933 1 4.54
CHEMBL4086755 1 4.49
CHEMBL4742119 1 4.46
CHEMBL4756815 1 4.43
CHEMBL4779689 1 4.12
CHEMBL4091194 1 4.12
CHEMBL4747550 1 4.08
CHEMBL7976 CHALCONE 1 4.07
CHEMBL4078900 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365190 IC50 = 4.65 nM 8.33
CHEMBL4780197 IC50 = 330.0 nM 6.48
CHEMBL4788400 IC50 = 580.0 nM 6.24
CHEMBL4797179 IC50 = 680.0 nM 6.17
CHEMBL4782276 IC50 = 830.0 nM 6.08
CHEMBL4748399 IC50 = 1690.0 nM 5.77
CHEMBL4757866 IC50 = 2090.0 nM 5.68
CHEMBL4744746 IC50 = 2520.0 nM 5.60
CHEMBL4752404 IC50 = 2540.0 nM 5.59
CHEMBL4740149 IC50 = 3320.0 nM 5.48
CHEMBL4776624 IC50 = 3500.0 nM 5.46
CHEMBL4761197 IC50 = 6940.0 nM 5.16
CHEMBL4745825 IC50 = 8610.0 nM 5.07
CHEMBL4747287 IC50 = 10420.0 nM 4.98
CHEMBL4751728 IC50 = 12360.0 nM 4.91
CHEMBL4778007 IC50 = 14790.0 nM 4.83
CHEMBL4080900 IC50 = 14800.0 nM 4.83
CHEMBL4160838 IC50 = 14890.0 nM 4.83
CHEMBL4780689 IC50 = 20660.0 nM 4.68
CHEMBL4765140 IC50 = 24810.0 nM 4.61
CHEMBL4750178 IC50 = 25090.0 nM 4.60
CHEMBL4098933 IC50 = 28930.0 nM 4.54
CHEMBL4086755 IC50 = 32670.0 nM 4.49
CHEMBL4742119 IC50 = 35010.0 nM 4.46
CHEMBL4756815 IC50 = 37150.0 nM 4.43
CHEMBL4779689 IC50 = 75380.0 nM 4.12
CHEMBL4091194 IC50 = 75580.0 nM 4.12
CHEMBL4747550 IC50 = 84090.0 nM 4.08
CHEMBL7976 CHALCONE IC50 = 84410.0 nM 4.07
CHEMBL4078900 IC50 > 100000.0 nM -
CHEMBL4785507 IC50 > 100000.0 nM -
CHEMBL4170979 IC50 > 100000.0 nM -