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Assay Detail

CHEMBL896284

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Binding
Displacement of [3H]methyllycaconitine from alpha7 nAChR in tsA201 cells co-expressed with Ric3
ChEMBL ↗
51
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 51 6.40 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510275 METHYLLYCACONITINE — 2 8.21
CHEMBL229998 — — 2 7.54
CHEMBL390135 — — 2 7.52
CHEMBL244561 — — 2 7.30
CHEMBL389120 — — 2 7.23
CHEMBL415570 — — 2 7.01
CHEMBL230952 — — 2 7.00
CHEMBL395727 — — 2 6.70
CHEMBL388049 — — 2 6.70
CHEMBL415569 — — 2 6.64
CHEMBL396705 — — 2 6.60
CHEMBL395960 — — 2 6.51
CHEMBL231056 — — 2 6.23
CHEMBL415568 — — 2 6.21
CHEMBL388047 — — 2 6.20
CHEMBL388046 — — 2 6.20
CHEMBL1180293 — — 2 6.00
CHEMBL388212 — — 2 6.00
CHEMBL382243 — — 2 5.90
CHEMBL388048 — — 2 5.80
CHEMBL231047 TOXIFERINE — 2 5.60
CHEMBL206666 — — 2 5.54
CHEMBL229999 — — 2 5.41
CHEMBL203627 — — 2 5.30
CHEMBL3 NICOTINE 4.0 2 5.00
CHEMBL18772 QUIPAZINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510275 METHYLLYCACONITINE Ki = 6.1 nM 8.21
CHEMBL510275 METHYLLYCACONITINE Ki = 6.31 nM 8.20
CHEMBL229998 — Ki = 29.0 nM 7.54
CHEMBL390135 — Ki = 30.0 nM 7.52
CHEMBL390135 — Ki = 31.62 nM 7.50
CHEMBL229998 — Ki = 31.62 nM 7.50
CHEMBL244561 — Ki = 50.12 nM 7.30
CHEMBL244561 — Ki = 55.0 nM 7.26
CHEMBL389120 — Ki = 59.0 nM 7.23
CHEMBL389120 — Ki = 63.1 nM 7.20
CHEMBL415570 — Ki = 98.0 nM 7.01
CHEMBL415570 — Ki = 100.0 nM 7.00
CHEMBL230952 — Ki = 100.0 nM 7.00
CHEMBL230952 — Ki = 100.0 nM 7.00
CHEMBL388049 — Ki = 200.0 nM 6.70
CHEMBL388049 — Ki = 199.53 nM 6.70
CHEMBL395727 — Ki = 199.53 nM 6.70
CHEMBL395727 — Ki = 210.0 nM 6.68
CHEMBL415569 — Ki = 230.0 nM 6.64
CHEMBL415569 — Ki = 251.19 nM 6.60
CHEMBL396705 — Ki = 250.0 nM 6.60
CHEMBL396705 — Ki = 251.19 nM 6.60
CHEMBL395960 — Ki = 310.0 nM 6.51
CHEMBL395960 — Ki = 316.23 nM 6.50
CHEMBL231056 — Ki = 590.0 nM 6.23
CHEMBL415568 — Ki = 620.0 nM 6.21
CHEMBL231056 — Ki = 630.96 nM 6.20
CHEMBL388047 — Ki = 630.96 nM 6.20
CHEMBL388046 — Ki = 630.96 nM 6.20
CHEMBL415568 — Ki = 630.96 nM 6.20
CHEMBL388046 — Ki = 640.0 nM 6.19
CHEMBL388047 — Ki = 710.0 nM 6.15
CHEMBL1180293 — Ki = 1000.0 nM 6.00
CHEMBL388212 — Ki = 1000.0 nM 6.00
CHEMBL1180293 — Ki = 1100.0 nM 5.96
CHEMBL388212 — Ki = 1100.0 nM 5.96
CHEMBL382243 — Ki = 1258.93 nM 5.90
CHEMBL382243 — Ki = 1300.0 nM 5.89
CHEMBL388048 — Ki = 1584.89 nM 5.80
CHEMBL388048 — Ki = 1700.0 nM 5.77
CHEMBL231047 TOXIFERINE Ki = 2511.89 nM 5.60
CHEMBL231047 TOXIFERINE Ki = 2600.0 nM 5.58
CHEMBL206666 — Ki = 2900.0 nM 5.54
CHEMBL206666 — Ki = 3162.28 nM 5.50
CHEMBL229999 — Ki = 3900.0 nM 5.41
CHEMBL229999 — Ki = 3981.07 nM 5.40
CHEMBL203627 — Ki = 5011.87 nM 5.30
CHEMBL203627 — Ki = 5400.0 nM 5.27
CHEMBL3 NICOTINE Ki = 10000.0 nM 5.00
CHEMBL3 NICOTINE Ki = 12000.0 nM 4.92