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Assay Detail

CHEMBL2384301

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

Binding
Inhibition of equine serum BuChE using S-butyrylthiocholine chloride 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 Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

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 4.70 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2380672 1 5.50
CHEMBL2380677 1 5.44
CHEMBL2380670 1 5.11
CHEMBL2380667 1 5.01
CHEMBL2380669 1 4.82
CHEMBL2380668 1 4.81
CHEMBL2380671 1 4.76
CHEMBL2380673 1 4.76
CHEMBL659 GALANTAMINE 4.0 1 4.71
CHEMBL2380674 1 4.70
CHEMBL156016 1 4.66
CHEMBL2380675 1 4.65
CHEMBL2332547 1 4.64
CHEMBL2380676 1 4.55
CHEMBL2332539 1 4.54
CHEMBL2332546 1 4.53
CHEMBL2332538 1 4.52
CHEMBL350032 1 4.51
CHEMBL454594 1 4.46
CHEMBL2332535 1 4.44
CHEMBL152675 1 4.42
CHEMBL2332537 1 4.29
CHEMBL2332536 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2380672 IC50 = 3130.0 nM 5.50
CHEMBL2380677 IC50 = 3640.0 nM 5.44
CHEMBL2380670 IC50 = 7820.0 nM 5.11
CHEMBL2380667 IC50 = 9650.0 nM 5.01
CHEMBL2380669 IC50 = 15110.0 nM 4.82
CHEMBL2380668 IC50 = 15440.0 nM 4.81
CHEMBL2380671 IC50 = 17420.0 nM 4.76
CHEMBL2380673 IC50 = 17210.0 nM 4.76
CHEMBL659 GALANTAMINE IC50 = 19340.0 nM 4.71
CHEMBL2380674 IC50 = 20140.0 nM 4.70
CHEMBL156016 IC50 = 22060.0 nM 4.66
CHEMBL2380675 IC50 = 22170.0 nM 4.65
CHEMBL2332547 IC50 = 23120.0 nM 4.64
CHEMBL2380676 IC50 = 28160.0 nM 4.55
CHEMBL2332539 IC50 = 28920.0 nM 4.54
CHEMBL2332546 IC50 = 29370.0 nM 4.53
CHEMBL2332538 IC50 = 30020.0 nM 4.52
CHEMBL350032 IC50 = 30580.0 nM 4.51
CHEMBL454594 IC50 = 35070.0 nM 4.46
CHEMBL2332535 IC50 = 36620.0 nM 4.44
CHEMBL152675 IC50 = 38190.0 nM 4.42
CHEMBL2332537 IC50 = 51160.0 nM 4.29
CHEMBL2332536 IC50 = 54040.0 nM 4.27