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Assay Detail

CHEMBL931480

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Binding
Displacement of [3H]EPI from Aplysia AChBP expressed in HEK293S cells by scintillation proximity assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aplysia
Cell Type HEK293S
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Mapping the elusive neonicotinoid binding site.
Tomizawa M, Talley TT, Maltby D, Durkin KA, Medzihradszky KF, Burlingame AL, Taylor P, Casida JE.
Proc Natl Acad Sci U S A (2007) 104 : 9075 -9080
PubMed 17485662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.44 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95904 1 8.77
CHEMBL451432 THIACLOPRID 1 8.08
CHEMBL6623 EPIBATIDINE 1 8.07
CHEMBL71046 DESCYANOTHIACLOPRID 1 8.07
CHEMBL265941 ACETAMIPRID 1 7.72
CHEMBL309804 DESNITROIMIDACLOPRID 1 7.36
CHEMBL259728 NITENPYRAM 1 6.75
CHEMBL406819 IMIDACLOPRID 1 6.75
CHEMBL3 NICOTINE 4.0 1 6.58
CHEMBL259727 CLOTHIANIDINE 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95904 Ki = 1.7 nM 8.77
CHEMBL451432 THIACLOPRID Ki = 8.4 nM 8.08
CHEMBL6623 EPIBATIDINE Ki = 8.6 nM 8.07
CHEMBL71046 DESCYANOTHIACLOPRID Ki = 8.5 nM 8.07
CHEMBL265941 ACETAMIPRID Ki = 19.0 nM 7.72
CHEMBL309804 DESNITROIMIDACLOPRID Ki = 44.0 nM 7.36
CHEMBL259728 NITENPYRAM Ki = 180.0 nM 6.75
CHEMBL406819 IMIDACLOPRID Ki = 180.0 nM 6.75
CHEMBL3 NICOTINE Ki = 260.0 nM 6.58
CHEMBL259727 CLOTHIANIDINE Ki = 574.0 nM 6.24