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Assay Detail

CHEMBL4844511

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

Binding
Inhibition of equine serum BuChE using butyrylthiocholine as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Tissue Serum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT<sub>6</sub> receptor with anti-aggregation properties against amyloid-beta and tau.
Wichur T, Pasieka A, Godyń J, Panek D, Góral I, Latacz G, Honkisz-Orzechowska E, Bucki A, Siwek A, Głuch-Lutwin M, Knez D, Brazzolotto X, Gobec S, Kołaczkowski M, Sabate R, Malawska B, Więckowska A.
Eur J Med Chem (2021) 225 : 113783 -113783
PubMed 34461507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.51 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4848231 1 8.66
CHEMBL4877482 1 8.39
CHEMBL4874513 1 8.03
CHEMBL95 TACRINE 4.0 1 7.82
CHEMBL4850051 1 7.73
CHEMBL4850546 1 7.61
CHEMBL4871964 1 6.41
CHEMBL4845823 1 6.34
CHEMBL4878361 1 6.28
CHEMBL4878383 1 6.23
CHEMBL4866788 1 6.15
CHEMBL4850488 1 6.05
CHEMBL4847532 1 5.97
CHEMBL4864206 1 5.97
CHEMBL4852099 1 5.88
CHEMBL4847373 1 5.78
CHEMBL502 DONEPEZIL 4.0 1 5.74
CHEMBL4863218 1 5.70
CHEMBL4868597 1 5.68
CHEMBL4854972 1 5.67
CHEMBL636 RIVASTIGMINE 4.0 1 5.66
CHEMBL4851595 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4848231 IC50 = 2.17 nM 8.66
CHEMBL4877482 IC50 = 4.07 nM 8.39
CHEMBL4874513 IC50 = 9.39 nM 8.03
CHEMBL95 TACRINE IC50 = 15.0 nM 7.82
CHEMBL4850051 IC50 = 18.76 nM 7.73
CHEMBL4850546 IC50 = 24.39 nM 7.61
CHEMBL4871964 IC50 = 393.7 nM 6.41
CHEMBL4845823 IC50 = 454.5 nM 6.34
CHEMBL4878361 IC50 = 527.9 nM 6.28
CHEMBL4878383 IC50 = 585.7 nM 6.23
CHEMBL4866788 IC50 = 701.4 nM 6.15
CHEMBL4850488 IC50 = 887.4 nM 6.05
CHEMBL4847532 IC50 = 1075.0 nM 5.97
CHEMBL4864206 IC50 = 1067.0 nM 5.97
CHEMBL4852099 IC50 = 1304.0 nM 5.88
CHEMBL4847373 IC50 = 1661.0 nM 5.78
CHEMBL502 DONEPEZIL IC50 = 1830.0 nM 5.74
CHEMBL4863218 IC50 = 1991.0 nM 5.70
CHEMBL4868597 IC50 = 2071.0 nM 5.68
CHEMBL4854972 IC50 = 2118.0 nM 5.67
CHEMBL636 RIVASTIGMINE IC50 = 2195.0 nM 5.66
CHEMBL4851595 IC50 = 4263.0 nM 5.37