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Assay Detail

CHEMBL2410352

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

Binding
Displacement of [3H]Epibatidine from human alpha7 nACHR expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor.
Mazurov AA, Kombo DC, Akireddy S, Murthy S, Hauser TA, Jordan KG, Gatto GJ, Yohannes D.
Bioorg Med Chem Lett (2013) 23 : 3927 -3934
PubMed 23692872 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 5.97 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2409491 1 8.30
CHEMBL2409487 1 8.00
CHEMBL2179962 1 7.70
CHEMBL2409489 1 7.52
CHEMBL2409486 1 7.00
CHEMBL2409492 1 7.00
CHEMBL3037927 1 6.85
CHEMBL2409490 1 6.52
CHEMBL2409485 1 6.52
CHEMBL2409482 1 6.46
CHEMBL2409488 1 6.40
CHEMBL2179961 1 6.08
CHEMBL2409480 1 6.00
CHEMBL2409478 1 5.85
CHEMBL2409496 1 5.80
CHEMBL2409483 1 5.72
CHEMBL2409479 1 5.57
CHEMBL3 NICOTINE 4.0 1 5.52
CHEMBL2409495 1 5.48
CHEMBL3037928 1 5.47
CHEMBL2409494 1 5.40
CHEMBL2409481 1 5.35
CHEMBL2179529 AZD1446 2.0 1 5.17
CHEMBL2409477 1 5.16
CHEMBL2409476 1 5.00
CHEMBL2407115 1 4.96
CHEMBL3037929 1 4.89
CHEMBL2409473 1 4.82
CHEMBL3037926 1 4.57
CHEMBL2409484 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2409491 Ki = 5.0 nM 8.30
CHEMBL2409487 Ki = 10.0 nM 8.00
CHEMBL2179962 Ki = 20.0 nM 7.70
CHEMBL2409489 Ki = 30.0 nM 7.52
CHEMBL2409486 Ki = 100.0 nM 7.00
CHEMBL2409492 Ki = 100.0 nM 7.00
CHEMBL3037927 Ki = 140.0 nM 6.85
CHEMBL2409490 Ki = 300.0 nM 6.52
CHEMBL2409485 Ki = 300.0 nM 6.52
CHEMBL2409482 Ki = 350.0 nM 6.46
CHEMBL2409488 Ki = 400.0 nM 6.40
CHEMBL2179961 Ki = 840.0 nM 6.08
CHEMBL2409480 Ki = 990.0 nM 6.00
CHEMBL2409478 Ki = 1400.0 nM 5.85
CHEMBL2409496 Ki = 1600.0 nM 5.80
CHEMBL2409483 Ki = 1900.0 nM 5.72
CHEMBL2409479 Ki = 2700.0 nM 5.57
CHEMBL3 NICOTINE Ki = 3000.0 nM 5.52
CHEMBL2409495 Ki = 3300.0 nM 5.48
CHEMBL3037928 Ki = 3400.0 nM 5.47
CHEMBL2409494 Ki = 4000.0 nM 5.40
CHEMBL2409481 Ki = 4500.0 nM 5.35
CHEMBL2179529 AZD1446 Ki = 6700.0 nM 5.17
CHEMBL2409477 Ki = 6900.0 nM 5.16
CHEMBL2409476 Ki = 10000.0 nM 5.00
CHEMBL2407115 Ki = 11000.0 nM 4.96
CHEMBL3037929 Ki = 13000.0 nM 4.89
CHEMBL2409473 Ki = 15000.0 nM 4.82
CHEMBL3037926 Ki = 27000.0 nM 4.57
CHEMBL2409484 Ki = 100000.0 nM 4.00
CHEMBL2409493 Ki - -
CHEMBL2409497 Ki - -
CHEMBL2409498 Ki - -
CHEMBL2409472 Ki - -
CHEMBL2409474 Ki - -
CHEMBL2409475 Ki - -