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Assay Detail

CHEMBL1020766

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

Binding
Displacement of [3H]epibatidine from alpha4beta2 nAChR expressed in HEK293 cells
43
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).
Hansen CP, Jensen AA, Balle T, Bitsch-Jensen K, Hassan MM, Liljefors T, Frølund B.
Bioorg Med Chem Lett (2009) 19 : 87 -91
PubMed 19027295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 5.74 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL466400 1 7.89
CHEMBL451633 2 7.44
CHEMBL466399 2 7.32
CHEMBL448084 2 7.04
CHEMBL500318 2 6.90
CHEMBL501227 2 6.70
CHEMBL468697 2 6.54
CHEMBL445169 2 5.96
CHEMBL468903 2 5.82
CHEMBL479622 2 5.80
CHEMBL480797 2 5.80
CHEMBL449334 2 5.72
CHEMBL480798 2 5.44
CHEMBL480799 2 5.20
CHEMBL503940 2 5.20
CHEMBL479623 2 5.01
CHEMBL499575 2 4.92
CHEMBL466398 2 4.64
CHEMBL479429 2 4.50
CHEMBL479015 2 4.40
CHEMBL457965 2 4.00
CHEMBL449566 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL466400 Ki = 13.0 nM 7.89
CHEMBL451633 Ki = 36.0 nM 7.44
CHEMBL451633 Ki = 39.81 nM 7.40
CHEMBL466399 Ki = 48.0 nM 7.32
CHEMBL466399 Ki = 50.12 nM 7.30
CHEMBL448084 Ki = 91.0 nM 7.04
CHEMBL448084 Ki = 100.0 nM 7.00
CHEMBL500318 Ki = 125.89 nM 6.90
CHEMBL500318 Ki = 130.0 nM 6.89
CHEMBL501227 Ki = 200.0 nM 6.70
CHEMBL501227 Ki = 199.53 nM 6.70
CHEMBL468697 Ki = 290.0 nM 6.54
CHEMBL468697 Ki = 316.23 nM 6.50
CHEMBL445169 Ki = 1100.0 nM 5.96
CHEMBL468903 Ki = 1500.0 nM 5.82
CHEMBL479622 Ki = 1600.0 nM 5.80
CHEMBL480797 Ki = 1600.0 nM 5.80
CHEMBL479622 Ki = 1584.89 nM 5.80
CHEMBL468903 Ki = 1584.89 nM 5.80
CHEMBL480797 Ki = 1584.89 nM 5.80
CHEMBL449334 Ki = 1900.0 nM 5.72
CHEMBL449334 Ki = 1995.26 nM 5.70
CHEMBL480798 Ki = 3600.0 nM 5.44
CHEMBL480798 Ki = 3981.07 nM 5.40
CHEMBL503940 Ki = 6309.57 nM 5.20
CHEMBL480799 Ki = 6309.57 nM 5.20
CHEMBL480799 Ki = 6500.0 nM 5.19
CHEMBL503940 Ki = 6600.0 nM 5.18
CHEMBL479623 Ki = 9800.0 nM 5.01
CHEMBL445169 Ki = 10000.0 nM 5.00
CHEMBL479623 Ki = 10000.0 nM 5.00
CHEMBL499575 Ki = 12000.0 nM 4.92
CHEMBL499575 Ki = 12589.25 nM 4.90
CHEMBL466398 Ki = 23000.0 nM 4.64
CHEMBL466398 Ki = 25118.86 nM 4.60
CHEMBL479429 Ki = 31622.78 nM 4.50
CHEMBL479429 Ki = 35000.0 nM 4.46
CHEMBL479015 Ki = 39810.72 nM 4.40
CHEMBL479015 Ki = 41000.0 nM 4.39
CHEMBL457965 Ki = 100000.0 nM 4.00
CHEMBL457965 Ki = 100000.0 nM 4.00
CHEMBL449566 Ki = 316227.77 nM -
CHEMBL449566 Ki = 300000.0 nM -