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Assay Detail

CHEMBL986292

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

Binding
Inhibition of human plasma BuchE by Ellman's method
27
Total Activities
27
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 Autocuration

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
Carolan CG, Dillon GP, Gaynor JM, Reidy S, Ryder SA, Khan D, Marquez JF, Gilmer JF.
J Med Chem (2008) 51 : 6400 -6409
PubMed 18817366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.62 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523830 1 8.37
CHEMBL492635 1 8.22
CHEMBL523005 1 7.92
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.55
CHEMBL492482 1 7.55
CHEMBL492898 1 7.50
CHEMBL445695 1 7.29
CHEMBL492283 1 7.24
CHEMBL494684 1 7.14
CHEMBL521810 1 7.14
CHEMBL492481 1 7.06
CHEMBL492233 1 6.86
CHEMBL492432 1 6.48
CHEMBL492636 1 6.45
CHEMBL494519 1 6.19
CHEMBL523500 1 6.17
CHEMBL521666 1 6.16
CHEMBL494887 TETRAISOPROPYL PYROPHOSPHORAMIDE 1 6.13
CHEMBL494520 1 6.05
CHEMBL493672 1 6.01
CHEMBL521852 1 5.60
CHEMBL492430 1 5.55
CHEMBL524046 1 5.43
CHEMBL494518 1 5.41
CHEMBL493460 1 5.39
CHEMBL492179 1 5.29
CHEMBL464538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523830 IC50 = 4.3 nM 8.37
CHEMBL492635 IC50 = 6.0 nM 8.22
CHEMBL523005 IC50 = 12.0 nM 7.92
CHEMBL94 PHYSOSTIGMINE IC50 = 28.0 nM 7.55
CHEMBL492482 IC50 = 28.0 nM 7.55
CHEMBL492898 IC50 = 32.0 nM 7.50
CHEMBL445695 IC50 = 51.0 nM 7.29
CHEMBL492283 IC50 = 57.0 nM 7.24
CHEMBL494684 IC50 = 72.0 nM 7.14
CHEMBL521810 IC50 = 73.0 nM 7.14
CHEMBL492481 IC50 = 88.0 nM 7.06
CHEMBL492233 IC50 = 137.0 nM 6.86
CHEMBL492432 IC50 = 334.0 nM 6.48
CHEMBL492636 IC50 = 359.0 nM 6.45
CHEMBL494519 IC50 = 639.0 nM 6.19
CHEMBL523500 IC50 = 669.0 nM 6.17
CHEMBL521666 IC50 = 700.0 nM 6.16
CHEMBL494887 TETRAISOPROPYL PYROPHOSPHORAMIDE IC50 = 733.0 nM 6.13
CHEMBL494520 IC50 = 894.0 nM 6.05
CHEMBL493672 IC50 = 980.0 nM 6.01
CHEMBL521852 IC50 = 2500.0 nM 5.60
CHEMBL492430 IC50 = 2800.0 nM 5.55
CHEMBL524046 IC50 = 3700.0 nM 5.43
CHEMBL494518 IC50 = 3900.0 nM 5.41
CHEMBL493460 IC50 = 4100.0 nM 5.39
CHEMBL492179 IC50 = 5100.0 nM 5.29
CHEMBL464538 IC50 = 255000.0 nM -