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

CHEMBL1948414

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

Binding
Displacement of [3H]epibatidine from Aplysia californica acetylcholine binding protein expressed using baculoviral system after 1.5 hrs by scintillation counting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aplysia californica
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Soluble acetylcholine receptor (CHEMBL1944497)
Type SINGLE PROTEIN
Organism Aplysia californica

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 26 5.81 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122270 LOBELINE 2.0 1 8.60
CHEMBL1947053 1 7.50
CHEMBL1947058 1 7.00
CHEMBL1947056 1 6.80
CHEMBL1947055 1 6.80
CHEMBL1947206 1 6.70
CHEMBL1946189 1 6.20
CHEMBL1947061 1 6.20
CHEMBL1947060 1 6.10
CHEMBL1947057 1 6.10
CHEMBL1946187 1 6.00
CHEMBL1947054 1 6.00
CHEMBL1947059 1 5.70
CHEMBL3 NICOTINE 4.0 1 5.60
CHEMBL1947051 BENZOYL TROPINE 1 5.40
CHEMBL1947049 1 5.30
CHEMBL1946186 DEPTROPINE 2.0 1 5.20
CHEMBL1947062 1 5.10
CHEMBL1794606 1 5.00
CHEMBL1946188 1 5.00
CHEMBL1946185 1 5.00
CHEMBL1947047 1 4.90
CHEMBL1947052 1 4.80
CHEMBL1947050 1 4.80
CHEMBL1947205 1 4.70
CHEMBL1947048 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122270 LOBELINE Ki = 2.512 nM 8.60
CHEMBL1947053 Ki = 31.62 nM 7.50
CHEMBL1947058 Ki = 100.0 nM 7.00
CHEMBL1947056 Ki = 158.49 nM 6.80
CHEMBL1947055 Ki = 158.49 nM 6.80
CHEMBL1947206 Ki = 199.53 nM 6.70
CHEMBL1946189 Ki = 630.96 nM 6.20
CHEMBL1947061 Ki = 630.96 nM 6.20
CHEMBL1947060 Ki = 794.33 nM 6.10
CHEMBL1947057 Ki = 794.33 nM 6.10
CHEMBL1946187 Ki = 1000.0 nM 6.00
CHEMBL1947054 Ki = 1000.0 nM 6.00
CHEMBL1947059 Ki = 1995.26 nM 5.70
CHEMBL3 NICOTINE Ki = 2511.89 nM 5.60
CHEMBL1947051 BENZOYL TROPINE Ki = 3981.07 nM 5.40
CHEMBL1947049 Ki = 5011.87 nM 5.30
CHEMBL1946186 DEPTROPINE Ki = 6309.57 nM 5.20
CHEMBL1947062 Ki = 7943.28 nM 5.10
CHEMBL1794606 Ki = 10000.0 nM 5.00
CHEMBL1946188 Ki = 10000.0 nM 5.00
CHEMBL1946185 Ki = 10000.0 nM 5.00
CHEMBL1947047 Ki = 12589.25 nM 4.90
CHEMBL1947052 Ki = 15848.93 nM 4.80
CHEMBL1947050 Ki = 15848.93 nM 4.80
CHEMBL1947205 Ki = 19952.62 nM 4.70
CHEMBL1947048 Ki = 31622.78 nM 4.50