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

CHEMBL2188201

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

Binding
Displacement of [3H]GR113808 from 5HT4R in guinea pig striatal membranes
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL5017)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.
Dubost E, Dumas N, Fossey C, Magnelli R, Butt-Gueulle S, Ballandonne C, Caignard DH, Dulin F, Sopkova de-Oliveira Santos J, Millet P, Charnay Y, Rault S, Cailly T, Fabis F.
J Med Chem (2012) 55 : 9693 -9707
PubMed 23102207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.32 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181170 1 8.66
CHEMBL2181166 1 8.60
CHEMBL2181168 1 8.34
CHEMBL2181171 1 7.88
CHEMBL2181169 1 7.87
CHEMBL2181189 1 7.70
CHEMBL2181190 1 7.67
CHEMBL2181188 1 7.66
CHEMBL2181172 1 7.64
CHEMBL2181187 1 7.46
CHEMBL2177145 1 7.29
CHEMBL2181185 1 7.00
CHEMBL2181186 1 7.00
CHEMBL2181167 1 6.94
CHEMBL2181175 1 6.81
CHEMBL2181173 1 6.68
CHEMBL2181181 1 6.63
CHEMBL2181180 1 6.61
CHEMBL2181184 1 6.16
CHEMBL2181183 1 5.72
CHEMBL2181174 1 -
CHEMBL2181178 1 -
CHEMBL2181179 1 -
CHEMBL2181182 1 -
CHEMBL2181177 1 -
CHEMBL2181176 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181170 Ki = 2.2 nM 8.66
CHEMBL2181166 Ki = 2.5 nM 8.60
CHEMBL2181168 Ki = 4.6 nM 8.34
CHEMBL2181171 Ki = 13.1 nM 7.88
CHEMBL2181169 Ki = 13.5 nM 7.87
CHEMBL2181189 Ki = 20.1 nM 7.70
CHEMBL2181190 Ki = 21.6 nM 7.67
CHEMBL2181188 Ki = 21.9 nM 7.66
CHEMBL2181172 Ki = 22.8 nM 7.64
CHEMBL2181187 Ki = 35.0 nM 7.46
CHEMBL2177145 Ki = 51.5 nM 7.29
CHEMBL2181185 Ki = 101.0 nM 7.00
CHEMBL2181186 Ki = 100.0 nM 7.00
CHEMBL2181167 Ki = 115.0 nM 6.94
CHEMBL2181175 Ki = 154.0 nM 6.81
CHEMBL2181173 Ki = 209.0 nM 6.68
CHEMBL2181181 Ki = 233.0 nM 6.63
CHEMBL2181180 Ki = 246.0 nM 6.61
CHEMBL2181184 Ki = 691.0 nM 6.16
CHEMBL2181183 Ki = 1900.0 nM 5.72
CHEMBL2181174 Ki - -
CHEMBL2181178 Ki - -
CHEMBL2181179 Ki - -
CHEMBL2181182 Ki - -
CHEMBL2181177 Ki - -
CHEMBL2181176 Ki - -