Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL896286

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

Functional
Antagonist activity at human alpha-7 nAChR in tsA201 cells coexpressed with Ric3 by FMP assay
ChEMBL ↗
49
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type tsA201
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
Jensen AA, Zlotos DP, Liljefors T.
J Med Chem (2007) 50 : 4616 -4629
PubMed 17722904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 5.64 8.08
EC50 5 5.40 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510275 METHYLLYCACONITINE — 2 8.08
CHEMBL390135 — — 2 6.55
CHEMBL244561 — — 2 6.47
CHEMBL229998 — — 2 6.43
CHEMBL230952 — — 2 5.96
CHEMBL389120 — — 2 5.89
CHEMBL395727 — — 2 5.83
CHEMBL388048 — — 2 5.82
CHEMBL388212 — — 2 5.80
CHEMBL395960 — — 2 5.80
CHEMBL415568 — — 2 5.68
CHEMBL415569 — — 2 5.64
CHEMBL415570 — — 2 5.61
CHEMBL388049 — — 2 5.58
CHEMBL231056 — — 2 5.52
CHEMBL667 ACETYLCHOLINE 4.0 2 5.40
CHEMBL1180293 — — 2 5.39
CHEMBL396705 — — 2 5.35
CHEMBL231047 TOXIFERINE — 2 5.02
CHEMBL388046 — — 2 5.00
CHEMBL382243 — — 2 4.52
CHEMBL206666 — — 2 4.52
CHEMBL229999 — — 2 4.52
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 -
CHEMBL773 GLYCINE 4.0 1 -
CHEMBL39 SEROTONIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510275 METHYLLYCACONITINE IC50 = 8.318 nM 8.08
CHEMBL510275 METHYLLYCACONITINE IC50 = 8.3 nM 8.08
CHEMBL390135 — IC50 = 280.0 nM 6.55
CHEMBL390135 — IC50 = 281.84 nM 6.55
CHEMBL244561 — IC50 = 338.84 nM 6.47
CHEMBL244561 — IC50 = 340.0 nM 6.47
CHEMBL229998 — IC50 = 370.0 nM 6.43
CHEMBL229998 — IC50 = 371.54 nM 6.43
CHEMBL230952 — IC50 = 1100.0 nM 5.96
CHEMBL230952 — IC50 = 1148.15 nM 5.94
CHEMBL389120 — IC50 = 1300.0 nM 5.89
CHEMBL389120 — IC50 = 1318.26 nM 5.88
CHEMBL395727 — IC50 = 1479.11 nM 5.83
CHEMBL395727 — IC50 = 1500.0 nM 5.82
CHEMBL388048 — IC50 = 1500.0 nM 5.82
CHEMBL388048 — IC50 = 1513.56 nM 5.82
CHEMBL395960 — IC50 = 1600.0 nM 5.80
CHEMBL388212 — IC50 = 1584.89 nM 5.80
CHEMBL388212 — IC50 = 1600.0 nM 5.80
CHEMBL395960 — IC50 = 1621.81 nM 5.79
CHEMBL415568 — IC50 = 2089.3 nM 5.68
CHEMBL415568 — IC50 = 2100.0 nM 5.68
CHEMBL415569 — IC50 = 2300.0 nM 5.64
CHEMBL415569 — IC50 = 2344.23 nM 5.63
CHEMBL415570 — IC50 = 2454.71 nM 5.61
CHEMBL415570 — IC50 = 2500.0 nM 5.60
CHEMBL388049 — IC50 = 2630.27 nM 5.58
CHEMBL388049 — IC50 = 2600.0 nM 5.58
CHEMBL231056 — IC50 = 3019.95 nM 5.52
CHEMBL231056 — IC50 = 3000.0 nM 5.52
CHEMBL667 ACETYLCHOLINE EC50 = 3981.07 nM 5.40
CHEMBL667 ACETYLCHOLINE EC50 = 4000.0 nM 5.40
CHEMBL1180293 — IC50 = 4100.0 nM 5.39
CHEMBL1180293 — IC50 = 4073.8 nM 5.39
CHEMBL396705 — IC50 = 4500.0 nM 5.35
CHEMBL396705 — IC50 = 4466.84 nM 5.35
CHEMBL231047 TOXIFERINE IC50 = 9500.0 nM 5.02
CHEMBL231047 TOXIFERINE IC50 = 9549.93 nM 5.02
CHEMBL388046 — IC50 = 10000.0 nM 5.00
CHEMBL388046 — IC50 = 10471.29 nM 4.98
CHEMBL206666 — IC50 = 30000.0 nM 4.52
CHEMBL382243 — IC50 = 30000.0 nM 4.52
CHEMBL229999 — IC50 = 30000.0 nM 4.52
CHEMBL382243 — IC50 = 100000.0 nM 4.00
CHEMBL229999 — IC50 = 100000.0 nM 4.00
CHEMBL206666 — IC50 = 100000.0 nM 4.00
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 - — -
CHEMBL773 GLYCINE EC50 - — -
CHEMBL39 SEROTONIN EC50 - — -