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Assay Detail

CHEMBL1948415

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Binding
Displacement of [3H]MLA from nAChR alpha7 receptor in human SH-SY5Y cells by scintillation counting
26
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.
Edink E, Akdemir A, Jansen C, van Elk R, Zuiderveld O, de Kanter FJ, van Muijlwijk-Koezen JE, Smit AB, Leurs R, de Esch IJ.
Bioorg Med Chem Lett (2012) 22 : 1448 -1454
PubMed 22243960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.11 6.00
pKi 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946187 1 6.00
CHEMBL3 NICOTINE 4.0 1 6.00
CHEMBL1946189 1 5.80
CHEMBL1947049 1 5.50
CHEMBL1947054 1 5.30
CHEMBL1947055 1 5.20
CHEMBL122270 LOBELINE 2.0 1 5.10
CHEMBL1947053 1 5.10
CHEMBL1947059 1 5.00
CHEMBL1947206 1 4.90
CHEMBL1947205 1 4.90
CHEMBL1947056 1 4.90
CHEMBL1946188 1 4.90
CHEMBL1947051 BENZOYL TROPINE 1 4.80
CHEMBL1947062 1 4.80
CHEMBL1947047 1 4.70
CHEMBL1947061 1 4.60
CHEMBL1947048 1 4.40
CHEMBL1947052 1 -
CHEMBL1947050 1 -
CHEMBL1947057 1 -
CHEMBL1947058 1 -
CHEMBL1794606 1 -
CHEMBL1947060 1 -
CHEMBL1946186 DEPTROPINE 2.0 1 -
CHEMBL1946185 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946187 Ki = 1000.0 nM 6.00
CHEMBL3 NICOTINE Ki = 1000.0 nM 6.00
CHEMBL1946189 Ki = 1584.89 nM 5.80
CHEMBL1947049 Ki = 3162.28 nM 5.50
CHEMBL1947054 Ki = 5011.87 nM 5.30
CHEMBL1947055 Ki = 6309.57 nM 5.20
CHEMBL122270 LOBELINE Ki = 7943.28 nM 5.10
CHEMBL1947053 Ki = 7943.28 nM 5.10
CHEMBL1947059 Ki = 10000.0 nM 5.00
CHEMBL1947206 Ki = 12589.25 nM 4.90
CHEMBL1947205 Ki = 12589.25 nM 4.90
CHEMBL1947056 Ki = 12589.25 nM 4.90
CHEMBL1946188 Ki = 12589.25 nM 4.90
CHEMBL1947051 BENZOYL TROPINE Ki = 15848.93 nM 4.80
CHEMBL1947062 Ki = 15848.93 nM 4.80
CHEMBL1947047 Ki = 19952.62 nM 4.70
CHEMBL1947061 Ki = 25118.86 nM 4.60
CHEMBL1947048 Ki = 39810.72 nM 4.40
CHEMBL1947052 pKi - -
CHEMBL1947050 pKi - -
CHEMBL1947057 pKi - -
CHEMBL1947058 pKi - -
CHEMBL1794606 pKi - -
CHEMBL1947060 pKi - -
CHEMBL1946186 DEPTROPINE pKi - -
CHEMBL1946185 pKi - -