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Assay Detail

CHEMBL641885

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Binding
Inhibition of rat acetylcholinesterase (AChE)
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.
Rampa A, Bisi A, Valenti P, Recanatini M, Cavalli A, Andrisano V, Cavrini V, Fin L, Buriani A, Giusti P.
J Med Chem (1998) 41 : 3976 -3986
PubMed 9767635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.80 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340427 XANTHOSTIGMINE 1 9.52
CHEMBL128202 1 9.25
CHEMBL131579 1 9.15
CHEMBL337999 1 9.09
CHEMBL131827 1 8.96
CHEMBL128260 1 8.55
CHEMBL131219 1 8.40
CHEMBL128471 1 8.24
CHEMBL340625 1 8.24
CHEMBL339039 1 8.07
CHEMBL128618 1 8.05
CHEMBL130918 1 8.05
CHEMBL128863 1 7.89
CHEMBL440526 1 7.89
CHEMBL128551 1 7.85
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.85
CHEMBL128552 1 7.68
CHEMBL336297 1 7.55
CHEMBL128043 1 7.51
CHEMBL130847 1 7.44
CHEMBL129753 1 7.43
CHEMBL128390 1 7.38
CHEMBL132110 1 7.17
CHEMBL128452 1 7.16
CHEMBL128780 1 7.00
CHEMBL131411 1 7.00
CHEMBL131253 1 7.00
CHEMBL127960 1 6.80
CHEMBL129577 1 6.77
CHEMBL128392 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340427 XANTHOSTIGMINE IC50 = 0.3 nM 9.52
CHEMBL128202 IC50 = 0.56 nM 9.25
CHEMBL131579 IC50 = 0.7 nM 9.15
CHEMBL337999 IC50 = 0.82 nM 9.09
CHEMBL131827 IC50 = 1.1 nM 8.96
CHEMBL128260 IC50 = 2.8 nM 8.55
CHEMBL131219 IC50 = 4.0 nM 8.40
CHEMBL128471 IC50 = 5.7 nM 8.24
CHEMBL340625 IC50 = 5.7 nM 8.24
CHEMBL339039 IC50 = 8.6 nM 8.07
CHEMBL128618 IC50 = 8.9 nM 8.05
CHEMBL130918 IC50 = 8.9 nM 8.05
CHEMBL128863 IC50 = 13.0 nM 7.89
CHEMBL440526 IC50 = 13.0 nM 7.89
CHEMBL128551 IC50 = 14.0 nM 7.85
CHEMBL94 PHYSOSTIGMINE IC50 = 14.0 nM 7.85
CHEMBL128552 IC50 = 21.0 nM 7.68
CHEMBL336297 IC50 = 28.0 nM 7.55
CHEMBL128043 IC50 = 31.0 nM 7.51
CHEMBL130847 IC50 = 36.0 nM 7.44
CHEMBL129753 IC50 = 37.0 nM 7.43
CHEMBL128390 IC50 = 42.0 nM 7.38
CHEMBL132110 IC50 = 68.0 nM 7.17
CHEMBL128452 IC50 = 70.0 nM 7.16
CHEMBL128780 IC50 = 100.0 nM 7.00
CHEMBL131411 IC50 = 100.0 nM 7.00
CHEMBL131253 IC50 = 100.0 nM 7.00
CHEMBL127960 IC50 = 160.0 nM 6.80
CHEMBL129577 IC50 = 170.0 nM 6.77
CHEMBL128392 IC50 = 250.0 nM 6.60
CHEMBL421282 IC50 = 400.0 nM 6.40