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Assay Detail

CHEMBL2384302

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

Binding
Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins by Ellman's method
23
Total Activities
23
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

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A facile chemo-, regio- and stereoselective synthesis and cholinesterase inhibitory activity of spirooxindole-pyrrolizine-piperidine hybrids.
Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Perumal S, Razak IA.
Bioorg Med Chem Lett (2013) 23 : 2979 -2983
PubMed 23570788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 4.98 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL659 GALANTAMINE 4.0 1 5.68
CHEMBL2380674 1 5.48
CHEMBL2380676 1 5.47
CHEMBL2380673 1 5.37
CHEMBL2380671 1 5.29
CHEMBL2380667 1 5.24
CHEMBL2380675 1 5.12
CHEMBL2332539 1 5.06
CHEMBL2332537 1 5.01
CHEMBL2380669 1 4.95
CHEMBL2332536 1 4.93
CHEMBL2332547 1 4.86
CHEMBL2380670 1 4.84
CHEMBL350032 1 4.82
CHEMBL2380668 1 4.80
CHEMBL2332546 1 4.80
CHEMBL2332535 1 4.79
CHEMBL2332538 1 4.76
CHEMBL156016 1 4.75
CHEMBL454594 1 4.74
CHEMBL152675 1 4.66
CHEMBL2380677 1 4.65
CHEMBL2380672 1 4.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL659 GALANTAMINE IC50 = 2090.0 nM 5.68
CHEMBL2380674 IC50 = 3330.0 nM 5.48
CHEMBL2380676 IC50 = 3360.0 nM 5.47
CHEMBL2380673 IC50 = 4280.0 nM 5.37
CHEMBL2380671 IC50 = 5080.0 nM 5.29
CHEMBL2380667 IC50 = 5810.0 nM 5.24
CHEMBL2380675 IC50 = 7600.0 nM 5.12
CHEMBL2332539 IC50 = 8720.0 nM 5.06
CHEMBL2332537 IC50 = 9760.0 nM 5.01
CHEMBL2380669 IC50 = 11200.0 nM 4.95
CHEMBL2332536 IC50 = 11810.0 nM 4.93
CHEMBL2332547 IC50 = 13840.0 nM 4.86
CHEMBL2380670 IC50 = 14520.0 nM 4.84
CHEMBL350032 IC50 = 15120.0 nM 4.82
CHEMBL2380668 IC50 = 15720.0 nM 4.80
CHEMBL2332546 IC50 = 15750.0 nM 4.80
CHEMBL2332535 IC50 = 16320.0 nM 4.79
CHEMBL2332538 IC50 = 17390.0 nM 4.76
CHEMBL156016 IC50 = 17680.0 nM 4.75
CHEMBL454594 IC50 = 18060.0 nM 4.74
CHEMBL152675 IC50 = 22040.0 nM 4.66
CHEMBL2380677 IC50 = 22320.0 nM 4.65
CHEMBL2380672 IC50 = 29510.0 nM 4.53