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Assay Detail

CHEMBL4433402

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

Binding
Inhibition of human serum butyrylcholinesterase using BTCI as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.
Sharma P, Tripathi A, Tripathi PN, Prajapati SK, Seth A, Tripathi MK, Srivastava P, Tiwari V, Krishnamurthy S, Shrivastava SK.
Eur J Med Chem (2019) 167 : 510 -524
PubMed 30784883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.24 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL636 RIVASTIGMINE 4.0 1 5.96
CHEMBL502 DONEPEZIL 4.0 1 5.85
CHEMBL4583534 1 5.52
CHEMBL4443695 1 5.51
CHEMBL4587156 1 5.46
CHEMBL4091169 1 5.46
CHEMBL4575167 1 5.41
CHEMBL1424080 1 5.41
CHEMBL1348834 1 5.40
CHEMBL4526950 1 5.34
CHEMBL4449445 1 5.26
CHEMBL4568264 1 5.24
CHEMBL4435826 1 5.14
CHEMBL4452092 1 5.14
CHEMBL4442580 1 5.11
CHEMBL4591283 1 4.96
CHEMBL4440283 1 4.96
CHEMBL4453051 1 4.92
CHEMBL4447514 1 4.85
CHEMBL4467620 1 4.80
CHEMBL4443013 1 4.75
CHEMBL4556855 1 4.72
CHEMBL4566555 1 -
CHEMBL4444849 1 -
CHEMBL4537808 1 -
CHEMBL4454571 1 -
CHEMBL4566242 1 -
CHEMBL4518938 1 -
CHEMBL4568615 1 -
CHEMBL4561792 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL636 RIVASTIGMINE IC50 = 1100.0 nM 5.96
CHEMBL502 DONEPEZIL IC50 = 1400.0 nM 5.85
CHEMBL4583534 IC50 = 3000.0 nM 5.52
CHEMBL4443695 IC50 = 3100.0 nM 5.51
CHEMBL4587156 IC50 = 3500.0 nM 5.46
CHEMBL4091169 IC50 = 3500.0 nM 5.46
CHEMBL4575167 IC50 = 3900.0 nM 5.41
CHEMBL1424080 IC50 = 3900.0 nM 5.41
CHEMBL1348834 IC50 = 4000.0 nM 5.40
CHEMBL4526950 IC50 = 4600.0 nM 5.34
CHEMBL4449445 IC50 = 5500.0 nM 5.26
CHEMBL4568264 IC50 = 5800.0 nM 5.24
CHEMBL4435826 IC50 = 7200.0 nM 5.14
CHEMBL4452092 IC50 = 7300.0 nM 5.14
CHEMBL4442580 IC50 = 7800.0 nM 5.11
CHEMBL4440283 IC50 = 11000.0 nM 4.96
CHEMBL4591283 IC50 = 11000.0 nM 4.96
CHEMBL4453051 IC50 = 12000.0 nM 4.92
CHEMBL4447514 IC50 = 14000.0 nM 4.85
CHEMBL4467620 IC50 = 16000.0 nM 4.80
CHEMBL4443013 IC50 = 18000.0 nM 4.75
CHEMBL4556855 IC50 = 19000.0 nM 4.72
CHEMBL4566555 IC50 > 30000.0 nM -
CHEMBL4444849 IC50 > 30000.0 nM -
CHEMBL4537808 IC50 > 30000.0 nM -
CHEMBL4454571 IC50 > 30000.0 nM -
CHEMBL4566242 IC50 > 30000.0 nM -
CHEMBL4518938 IC50 > 30000.0 nM -
CHEMBL4568615 IC50 > 30000.0 nM -
CHEMBL4561792 IC50 > 30000.0 nM -
CHEMBL4458653 IC50 > 30000.0 nM -
CHEMBL4444968 IC50 > 30000.0 nM -