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Assay Detail

CHEMBL891276

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

Binding
Inhibition of BuChE in rat serum
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Serum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Butyrylcholinesterase (CHEMBL3403)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
He XC, Feng S, Wang ZF, Shi Y, Zheng S, Xia Y, Jiang H, Tang XC, Bai D.
Bioorg Med Chem (2007) 15 : 1394 -1408
PubMed 17126020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 4.43 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389579 1 5.46
CHEMBL389375 1 5.06
CHEMBL244230 1 4.89
CHEMBL395281 1 4.22
CHEMBL397232 1 4.20
CHEMBL241856 1 4.19
CHEMBL245080 1 4.19
CHEMBL395282 1 4.18
CHEMBL415423 1 4.17
CHEMBL395280 HUPERZINE A 2.0 1 4.15
CHEMBL440054 1 4.05
CHEMBL242068 1 -
CHEMBL438305 1 -
CHEMBL245081 1 -
CHEMBL267591 1 -
CHEMBL413241 1 -
CHEMBL413242 1 -
CHEMBL267836 1 -
CHEMBL413243 1 -
CHEMBL413244 1 -
CHEMBL389580 1 -
CHEMBL242755 1 -
CHEMBL263098 1 -
CHEMBL389779 1 -
CHEMBL413170 1 -
CHEMBL267606 1 -
CHEMBL244027 1 -
CHEMBL413018 1 -
CHEMBL413240 1 -
CHEMBL244026 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389579 IC50 = 3480.0 nM 5.46
CHEMBL389375 IC50 = 8650.0 nM 5.06
CHEMBL244230 IC50 = 12900.0 nM 4.89
CHEMBL395281 IC50 = 60000.0 nM 4.22
CHEMBL397232 IC50 = 63000.0 nM 4.20
CHEMBL241856 IC50 = 65000.0 nM 4.19
CHEMBL245080 IC50 = 64500.0 nM 4.19
CHEMBL395282 IC50 = 65400.0 nM 4.18
CHEMBL415423 IC50 = 67900.0 nM 4.17
CHEMBL395280 HUPERZINE A IC50 = 70200.0 nM 4.15
CHEMBL440054 IC50 = 88400.0 nM 4.05
CHEMBL245081 IC50 - -
CHEMBL389583 IC50 = 125000.0 nM -
CHEMBL438305 IC50 - -
CHEMBL242068 IC50 - -
CHEMBL263097 IC50 - -
CHEMBL397501 IC50 - -
CHEMBL395106 IC50 - -
CHEMBL395043 IC50 - -
CHEMBL395274 IC50 - -
CHEMBL389374 IC50 - -
CHEMBL395520 IC50 - -
CHEMBL245079 HUPERZINE B IC50 = 228000.0 nM -
CHEMBL244870 IC50 > 184000.0 nM -
CHEMBL395283 IC50 = 171000.0 nM -
CHEMBL389582 IC50 = 192000.0 nM -
CHEMBL267591 IC50 - -
CHEMBL413241 IC50 - -
CHEMBL413242 IC50 - -
CHEMBL267836 IC50 - -
CHEMBL413243 IC50 - -
CHEMBL413244 IC50 - -
CHEMBL389580 IC50 - -
CHEMBL242755 IC50 - -
CHEMBL263098 IC50 - -
CHEMBL389779 IC50 - -
CHEMBL413170 IC50 - -
CHEMBL267606 IC50 - -
CHEMBL244027 IC50 - -
CHEMBL413018 IC50 - -
CHEMBL413240 IC50 - -
CHEMBL244026 IC50 - -