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Assay Detail

CHEMBL756006

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Binding
Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.
Wei ZL, Petukhov PA, Xiao Y, Tückmantel W, George C, Kellar KJ, Kozikowski AP.
J Med Chem (2003) 46 : 921 -924
PubMed 12620069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.93 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 10.21
CHEMBL3 NICOTINE 4.0 1 8.00
CHEMBL425135 1 7.14
CHEMBL170873 1 6.53
CHEMBL367641 1 5.16
CHEMBL173610 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.061 nM 10.21
CHEMBL3 NICOTINE Ki = 10.0 nM 8.00
CHEMBL425135 Ki = 73.0 nM 7.14
CHEMBL170873 Ki = 295.0 nM 6.53
CHEMBL367641 Ki = 6990.0 nM 5.16
CHEMBL173610 Ki = 29200.0 nM 4.54