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Assay Detail

CHEMBL898044

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

Binding
Inhibition of human plasma BuChE activity
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine.
Darvesh S, McDonald RS, Darvesh KV, Mataija D, Conrad S, Gomez G, Walsh R, Martin E.
Bioorg Med Chem (2007) 15 : 6367 -6378
PubMed 17681768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.16 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392577 1 8.46
CHEMBL241115 1 7.55
CHEMBL240899 1 7.06
CHEMBL241114 1 7.05
CHEMBL391727 1 6.66
CHEMBL394755 1 6.66
CHEMBL240261 1 6.40
CHEMBL240900 1 6.33
CHEMBL240045 1 6.25
CHEMBL239616 1 6.22
CHEMBL394753 1 6.21
CHEMBL239834 1 6.09
CHEMBL239617 1 5.89
CHEMBL239618 1 5.82
CHEMBL240469 1 5.77
CHEMBL240262 1 5.77
CHEMBL239401 1 5.72
CHEMBL397100 1 5.60
CHEMBL241558 1 5.57
CHEMBL397099 1 5.51
CHEMBL239400 1 5.24
CHEMBL240047 1 5.21
CHEMBL397101 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392577 Ki = 3.5 nM 8.46
CHEMBL241115 Ki = 28.0 nM 7.55
CHEMBL240899 Ki = 88.0 nM 7.06
CHEMBL241114 Ki = 90.0 nM 7.05
CHEMBL391727 Ki = 220.0 nM 6.66
CHEMBL394755 Ki = 220.0 nM 6.66
CHEMBL240261 Ki = 400.0 nM 6.40
CHEMBL240900 Ki = 470.0 nM 6.33
CHEMBL240045 Ki = 560.0 nM 6.25
CHEMBL239616 Ki = 600.0 nM 6.22
CHEMBL394753 Ki = 610.0 nM 6.21
CHEMBL239834 Ki = 820.0 nM 6.09
CHEMBL239617 Ki = 1300.0 nM 5.89
CHEMBL239618 Ki = 1500.0 nM 5.82
CHEMBL240469 Ki = 1700.0 nM 5.77
CHEMBL240262 Ki = 1700.0 nM 5.77
CHEMBL239401 Ki = 1900.0 nM 5.72
CHEMBL397100 Ki = 2500.0 nM 5.60
CHEMBL241558 Ki = 2700.0 nM 5.57
CHEMBL397099 Ki = 3100.0 nM 5.51
CHEMBL239400 Ki = 5800.0 nM 5.24
CHEMBL240047 Ki = 6200.0 nM 5.21
CHEMBL397101 Ki = 23000.0 nM 4.64