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Assay Detail

CHEMBL753099

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Binding
Potency to displace [3H]IMI binding to Nicotinic acetylcholine receptor from Drosophila head membranes
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Drosophila melanogaster
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors.
Zhang N, Tomizawa M, Casida JE.
J Med Chem (2002) 45 : 2832 -2840
PubMed 12061885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.12 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100491 1 9.92
CHEMBL97798 1 9.46
CHEMBL319510 1 9.14
CHEMBL95367 DEHYDROIMIDACLOPRID 1 9.07
CHEMBL95352 THIACLOPRID OLEFIN 1 8.85
CHEMBL406819 IMIDACLOPRID 1 8.66
CHEMBL98451 1 8.41
CHEMBL95531 1 7.89
CHEMBL97343 5-AZIDOIMIDACLOPRID 1 7.62
CHEMBL95904 1 7.55
CHEMBL72675 1 7.00
CHEMBL6623 EPIBATIDINE 1 6.66
CHEMBL318765 1 6.34
CHEMBL97016 1 6.27
CHEMBL319885 1 6.12
CHEMBL309804 DESNITROIMIDACLOPRID 1 6.10
CHEMBL3 NICOTINE 4.0 1 5.70
CHEMBL330079 1 5.50
CHEMBL327625 1 5.44
CHEMBL316493 1 5.24
CHEMBL317288 1 5.14
CHEMBL96405 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100491 Ki = 0.12 nM 9.92
CHEMBL97798 Ki = 0.35 nM 9.46
CHEMBL319510 Ki = 0.72 nM 9.14
CHEMBL95367 DEHYDROIMIDACLOPRID Ki = 0.85 nM 9.07
CHEMBL95352 THIACLOPRID OLEFIN Ki = 1.4 nM 8.85
CHEMBL406819 IMIDACLOPRID Ki = 2.2 nM 8.66
CHEMBL98451 Ki = 3.9 nM 8.41
CHEMBL95531 Ki = 13.0 nM 7.89
CHEMBL97343 5-AZIDOIMIDACLOPRID Ki = 24.0 nM 7.62
CHEMBL95904 Ki = 28.0 nM 7.55
CHEMBL72675 Ki = 100.0 nM 7.00
CHEMBL6623 EPIBATIDINE Ki = 220.0 nM 6.66
CHEMBL318765 Ki = 460.0 nM 6.34
CHEMBL97016 Ki = 540.0 nM 6.27
CHEMBL319885 Ki = 750.0 nM 6.12
CHEMBL309804 DESNITROIMIDACLOPRID Ki = 800.0 nM 6.10
CHEMBL3 NICOTINE Ki = 2000.0 nM 5.70
CHEMBL330079 Ki = 3200.0 nM 5.50
CHEMBL327625 Ki = 3600.0 nM 5.44
CHEMBL316493 Ki = 5700.0 nM 5.24
CHEMBL317288 Ki = 7200.0 nM 5.14
CHEMBL96405 Ki = 30000.0 nM 4.52