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Assay Detail

CHEMBL2345676

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

Binding
Inhibition of AChE (unknown origin) using acetylthiocholine iodide substrate by Ellman's method based spectrophotometry
34
Total Activities
34
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

Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors.
Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Perumal S, Wahab HA, Bing CS.
Bioorg Med Chem (2013) 21 : 1696 -1707
PubMed 23454132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 4.88 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL659 GALANTAMINE 4.0 1 5.68
CHEMBL2332979 1 5.47
CHEMBL2332977 1 5.39
CHEMBL2332976 1 5.22
CHEMBL2332545 1 5.17
CHEMBL2332531 1 5.16
CHEMBL2332541 1 5.10
CHEMBL2332539 1 5.06
CHEMBL2332537 1 5.01
CHEMBL2332542 1 4.94
CHEMBL2332536 1 4.93
CHEMBL2332974 1 4.92
CHEMBL2332549 1 4.90
CHEMBL2332534 1 4.87
CHEMBL2332547 1 4.86
CHEMBL350032 1 4.82
CHEMBL2332546 1 4.80
CHEMBL2332550 1 4.80
CHEMBL2332535 1 4.79
CHEMBL2332548 1 4.76
CHEMBL2332538 1 4.76
CHEMBL156016 1 4.75
CHEMBL454594 1 4.74
CHEMBL2332544 1 4.71
CHEMBL2332530 1 4.71
CHEMBL2332978 1 4.70
CHEMBL2332980 1 4.70
CHEMBL2332981 1 4.69
CHEMBL152675 1 4.66
CHEMBL2332540 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL659 GALANTAMINE IC50 = 2090.0 nM 5.68
CHEMBL2332979 IC50 = 3360.0 nM 5.47
CHEMBL2332977 IC50 = 4110.0 nM 5.39
CHEMBL2332976 IC50 = 5990.0 nM 5.22
CHEMBL2332545 IC50 = 6760.0 nM 5.17
CHEMBL2332531 IC50 = 6960.0 nM 5.16
CHEMBL2332541 IC50 = 7920.0 nM 5.10
CHEMBL2332539 IC50 = 8720.0 nM 5.06
CHEMBL2332537 IC50 = 9760.0 nM 5.01
CHEMBL2332542 IC50 = 11410.0 nM 4.94
CHEMBL2332536 IC50 = 11810.0 nM 4.93
CHEMBL2332974 IC50 = 11920.0 nM 4.92
CHEMBL2332549 IC50 = 12470.0 nM 4.90
CHEMBL2332534 IC50 = 13640.0 nM 4.87
CHEMBL2332547 IC50 = 13840.0 nM 4.86
CHEMBL350032 IC50 = 15120.0 nM 4.82
CHEMBL2332550 IC50 = 15860.0 nM 4.80
CHEMBL2332546 IC50 = 15750.0 nM 4.80
CHEMBL2332535 IC50 = 16320.0 nM 4.79
CHEMBL2332548 IC50 = 17490.0 nM 4.76
CHEMBL2332538 IC50 = 17390.0 nM 4.76
CHEMBL156016 IC50 = 17680.0 nM 4.75
CHEMBL454594 IC50 = 18060.0 nM 4.74
CHEMBL2332544 IC50 = 19650.0 nM 4.71
CHEMBL2332530 IC50 = 19590.0 nM 4.71
CHEMBL2332978 IC50 = 20070.0 nM 4.70
CHEMBL2332980 IC50 = 19840.0 nM 4.70
CHEMBL2332981 IC50 = 20630.0 nM 4.69
CHEMBL152675 IC50 = 22040.0 nM 4.66
CHEMBL2332540 IC50 = 23670.0 nM 4.63
CHEMBL2332533 IC50 = 24580.0 nM 4.61
CHEMBL2332532 IC50 = 26600.0 nM 4.58
CHEMBL2332543 IC50 = 27450.0 nM 4.56
CHEMBL2332975 IC50 = 34370.0 nM 4.46