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Assay Detail

CHEMBL3788097

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

Binding
Agonist activity at human alpha7 nAChR expressed in xenopus oocytes preincubated for 10 mins followed by acetylcholine addition by patch clamp electrophysiological assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists.
Xue Y, Tang J, Ma X, Li Q, Xie B, Hao Y, Jin H, Wang K, Zhang G, Zhang L, Zhang L.
Eur J Med Chem (2016) 115 : 94 -108
PubMed 26994846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 5.38 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151572 ENCENICLINE 3.0 1 6.47
CHEMBL3786240 1 5.75
CHEMBL3785589 1 5.67
CHEMBL3786561 1 5.60
CHEMBL3787650 1 5.55
CHEMBL3787063 1 5.45
CHEMBL3786124 1 5.40
CHEMBL3787561 1 5.40
CHEMBL3787485 1 5.33
CHEMBL3786427 1 5.32
CHEMBL3786711 1 5.16
CHEMBL3786820 1 5.08
CHEMBL3786022 1 5.07
CHEMBL3785274 1 5.02
CHEMBL3786847 1 4.98
CHEMBL3787101 1 4.85
CHEMBL3786196 1 -
CHEMBL3786664 1 -
CHEMBL3787649 1 -
CHEMBL3785578 1 -
CHEMBL3786458 1 -
CHEMBL3785483 1 -
CHEMBL3786757 1 -
CHEMBL3787659 1 -
CHEMBL3787203 1 -
CHEMBL3786064 1 -
CHEMBL3786302 1 -
CHEMBL3786349 1 -
CHEMBL3786288 1 -
CHEMBL3786509 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151572 ENCENICLINE EC50 = 340.0 nM 6.47
CHEMBL3786240 EC50 = 1780.0 nM 5.75
CHEMBL3785589 EC50 = 2140.0 nM 5.67
CHEMBL3786561 EC50 = 2490.0 nM 5.60
CHEMBL3787650 EC50 = 2830.0 nM 5.55
CHEMBL3787063 EC50 = 3540.0 nM 5.45
CHEMBL3786124 EC50 = 3980.0 nM 5.40
CHEMBL3787561 EC50 = 3990.0 nM 5.40
CHEMBL3787485 EC50 = 4640.0 nM 5.33
CHEMBL3786427 EC50 = 4750.0 nM 5.32
CHEMBL3786711 EC50 = 6920.0 nM 5.16
CHEMBL3786820 EC50 = 8380.0 nM 5.08
CHEMBL3786022 EC50 = 8600.0 nM 5.07
CHEMBL3785274 EC50 = 9630.0 nM 5.02
CHEMBL3786847 EC50 = 10480.0 nM 4.98
CHEMBL3787101 EC50 = 14130.0 nM 4.85
CHEMBL3785383 EC50 > 20000.0 nM -
CHEMBL3786875 EC50 > 20000.0 nM -
CHEMBL3786604 EC50 > 20000.0 nM -
CHEMBL3786699 EC50 > 20000.0 nM -
CHEMBL3786717 EC50 > 20000.0 nM -
CHEMBL3787259 EC50 > 20000.0 nM -
CHEMBL3785700 EC50 > 20000.0 nM -
CHEMBL3785845 EC50 > 20000.0 nM -
CHEMBL3785097 EC50 > 20000.0 nM -
CHEMBL3787199 EC50 > 20000.0 nM -
CHEMBL3787676 EC50 > 20000.0 nM -
CHEMBL3786366 EC50 > 20000.0 nM -
CHEMBL3787675 EC50 > 20000.0 nM -
CHEMBL3787416 EC50 > 20000.0 nM -
CHEMBL3787585 EC50 > 20000.0 nM -
CHEMBL3785410 EC50 > 20000.0 nM -
CHEMBL3786253 EC50 > 20000.0 nM -
CHEMBL3786273 EC50 > 20000.0 nM -
CHEMBL3786509 EC50 > 20000.0 nM -
CHEMBL3786288 EC50 > 20000.0 nM -
CHEMBL3786349 EC50 > 20000.0 nM -
CHEMBL3786302 EC50 > 20000.0 nM -
CHEMBL3786064 EC50 > 20000.0 nM -
CHEMBL3787203 EC50 > 20000.0 nM -
CHEMBL3787659 EC50 > 20000.0 nM -
CHEMBL3786757 EC50 > 20000.0 nM -
CHEMBL3785483 EC50 > 20000.0 nM -
CHEMBL3786458 EC50 > 20000.0 nM -
CHEMBL3785578 EC50 > 20000.0 nM -
CHEMBL3787649 EC50 > 20000.0 nM -
CHEMBL3786664 EC50 > 20000.0 nM -
CHEMBL3786196 EC50 > 20000.0 nM -