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Assay Detail

CHEMBL5328237

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

Binding
Negative allosteric modulator activity at human Pancreatic lipase using DDAO-ol as fluorescent substrate preincubated for 3 mins followed by substrate addition measured after 20 mins by microplate reader assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Pancreatic triacylglycerol lipase (CHEMBL1812)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase.
Zhao Y, Zhang M, Hou X, Han J, Qin X, Yang Y, Song Y, Liu Z, Zhang Y, Xu Z, Jia Q, Li Y, Chen K, Li B, Zhu W, Ge G.
Bioorg Med Chem (2023) 91 : 117413 -117413
PubMed 37490786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.20 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175247 ORLISTAT 4.0 1 8.80
CHEMBL164 MYRICETIN 1 5.87
CHEMBL50 QUERCETIN 3.0 1 5.82
CHEMBL4641560 1 5.79
CHEMBL5410259 1 5.73
CHEMBL1631675 1 5.67
CHEMBL287542 RAFOXANIDE 2.0 1 5.60
CHEMBL204813 SANGGENON C 1 5.48
CHEMBL5423733 1 5.37
CHEMBL5419885 1 5.22
CHEMBL5413231 1 5.20
CHEMBL5405185 1 5.17
CHEMBL5439220 1 5.03
CHEMBL5402667 1 5.00
CHEMBL5399755 1 5.00
CHEMBL5420710 1 4.98
CHEMBL5430137 1 4.96
CHEMBL5436175 1 4.95
CHEMBL5396102 1 4.92
CHEMBL5428235 1 4.91
CHEMBL5412428 1 4.91
CHEMBL5404043 1 4.82
CHEMBL5409756 1 4.80
CHEMBL5418104 1 4.78
CHEMBL5404594 1 4.74
CHEMBL5409828 1 4.72
CHEMBL5432097 1 4.69
CHEMBL5412841 1 4.62
CHEMBL5413833 1 4.58
CHEMBL5432795 1 4.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175247 ORLISTAT IC50 = 1.57 nM 8.80
CHEMBL164 MYRICETIN IC50 = 1340.0 nM 5.87
CHEMBL50 QUERCETIN IC50 = 1530.0 nM 5.82
CHEMBL4641560 IC50 = 1630.0 nM 5.79
CHEMBL5410259 IC50 = 1860.0 nM 5.73
CHEMBL1631675 IC50 = 2130.0 nM 5.67
CHEMBL287542 RAFOXANIDE IC50 = 2520.0 nM 5.60
CHEMBL204813 SANGGENON C IC50 = 3280.0 nM 5.48
CHEMBL5423733 IC50 = 4270.0 nM 5.37
CHEMBL5419885 IC50 = 5990.0 nM 5.22
CHEMBL5413231 IC50 = 6270.0 nM 5.20
CHEMBL5405185 IC50 = 6750.0 nM 5.17
CHEMBL5439220 IC50 = 9240.0 nM 5.03
CHEMBL5402667 IC50 = 9960.0 nM 5.00
CHEMBL5399755 IC50 = 10000.0 nM 5.00
CHEMBL5420710 IC50 = 10510.0 nM 4.98
CHEMBL5430137 IC50 = 11020.0 nM 4.96
CHEMBL5436175 IC50 = 11360.0 nM 4.95
CHEMBL5396102 IC50 = 12040.0 nM 4.92
CHEMBL5428235 IC50 = 12360.0 nM 4.91
CHEMBL5412428 IC50 = 12380.0 nM 4.91
CHEMBL5404043 IC50 = 15000.0 nM 4.82
CHEMBL5409756 IC50 = 15750.0 nM 4.80
CHEMBL5418104 IC50 = 16670.0 nM 4.78
CHEMBL5404594 IC50 = 18270.0 nM 4.74
CHEMBL5409828 IC50 = 19070.0 nM 4.72
CHEMBL5432097 IC50 = 20410.0 nM 4.69
CHEMBL5412841 IC50 = 23710.0 nM 4.62
CHEMBL5413833 IC50 = 26320.0 nM 4.58
CHEMBL5432795 IC50 = 27360.0 nM 4.56
CHEMBL5415926 IC50 = 32660.0 nM 4.49
CHEMBL389507 OSALMID IC50 > 500000.0 nM -