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Assay Detail

CHEMBL894634

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

Functional
Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers.
Russo O, Berthouze M, Giner M, Soulier JL, Rivail L, Sicsic S, Lezoualc'h F, Jockers R, Berque-Bestel I.
J Med Chem (2007) 50 : 4482 -4492
PubMed 17676726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.80 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33884 1 9.30
CHEMBL286136 1 8.30
CHEMBL390205 1 8.15
CHEMBL2113284 1 8.10
CHEMBL371718 1 8.05
CHEMBL2113289 1 7.92
CHEMBL1162955 1 7.82
CHEMBL390202 1 7.82
CHEMBL2113285 1 7.75
CHEMBL2113288 1 7.72
CHEMBL390075 1 7.70
CHEMBL2113290 1 7.64
CHEMBL2113287 1 7.60
CHEMBL2113291 1 7.47
CHEMBL2113286 1 7.40
CHEMBL2113283 1 7.36
CHEMBL408379 1 7.30
CHEMBL2113160 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33884 Ki = 0.5 nM 9.30
CHEMBL286136 Ki = 5.0 nM 8.30
CHEMBL390205 Ki = 7.0 nM 8.15
CHEMBL2113284 Ki = 8.0 nM 8.10
CHEMBL371718 Ki = 9.0 nM 8.05
CHEMBL2113289 Ki = 12.0 nM 7.92
CHEMBL1162955 Ki = 15.0 nM 7.82
CHEMBL390202 Ki = 15.0 nM 7.82
CHEMBL2113285 Ki = 18.0 nM 7.75
CHEMBL2113288 Ki = 19.0 nM 7.72
CHEMBL390075 Ki = 20.0 nM 7.70
CHEMBL2113290 Ki = 23.0 nM 7.64
CHEMBL2113287 Ki = 25.0 nM 7.60
CHEMBL2113291 Ki = 34.0 nM 7.47
CHEMBL2113286 Ki = 40.0 nM 7.40
CHEMBL2113283 Ki = 44.0 nM 7.36
CHEMBL408379 Ki = 50.0 nM 7.30
CHEMBL2113160 Ki = 113.0 nM 6.95