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Assay Detail

CHEMBL882452

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

Binding
Binding affinity for 5-HT4 receptor using [3H]GR-113808
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies.
Soulier JL, Russo O, Giner M, Rivail L, Berthouze M, Ongeri S, Maigret B, Fischmeister R, Lezoualc'h F, Sicsic S, Berque-Bestel I.
J Med Chem (2005) 48 : 6220 -6228
PubMed 16190749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.79 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198271 1 8.52
CHEMBL286136 1 8.30
CHEMBL198668 1 8.30
CHEMBL197745 1 8.30
CHEMBL197752 1 8.30
CHEMBL370796 1 8.22
CHEMBL198719 1 8.15
CHEMBL196633 1 8.10
CHEMBL370646 1 8.10
CHEMBL370227 1 8.05
CHEMBL372479 1 8.05
CHEMBL370181 1 8.00
CHEMBL370182 1 7.96
CHEMBL382543 1 7.96
CHEMBL198052 1 7.89
CHEMBL197965 1 7.89
CHEMBL198921 1 7.89
CHEMBL198504 1 7.85
CHEMBL199150 1 7.80
CHEMBL189580 1 7.80
CHEMBL371718 1 7.75
CHEMBL371707 1 7.72
CHEMBL390075 1 7.70
CHEMBL197751 1 7.68
CHEMBL2113157 1 7.62
CHEMBL2113158 1 7.51
CHEMBL2113159 1 7.43
CHEMBL198226 1 7.33
CHEMBL408379 1 7.30
CHEMBL2113160 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198271 Ki = 3.0 nM 8.52
CHEMBL286136 Ki = 5.0 nM 8.30
CHEMBL198668 Ki = 5.0 nM 8.30
CHEMBL197745 Ki = 5.0 nM 8.30
CHEMBL197752 Ki = 5.0 nM 8.30
CHEMBL370796 Ki = 6.0 nM 8.22
CHEMBL198719 Ki = 7.0 nM 8.15
CHEMBL196633 Ki = 8.0 nM 8.10
CHEMBL370646 Ki = 8.0 nM 8.10
CHEMBL370227 Ki = 9.0 nM 8.05
CHEMBL372479 Ki = 9.0 nM 8.05
CHEMBL370181 Ki = 10.0 nM 8.00
CHEMBL370182 Ki = 11.0 nM 7.96
CHEMBL382543 Ki = 11.0 nM 7.96
CHEMBL197965 Ki = 13.0 nM 7.89
CHEMBL198921 Ki = 13.0 nM 7.89
CHEMBL198052 Ki = 13.0 nM 7.89
CHEMBL198504 Ki = 14.0 nM 7.85
CHEMBL199150 Ki = 16.0 nM 7.80
CHEMBL189580 Ki = 16.0 nM 7.80
CHEMBL371718 Ki = 18.0 nM 7.75
CHEMBL371707 Ki = 19.0 nM 7.72
CHEMBL390075 Ki = 20.0 nM 7.70
CHEMBL197751 Ki = 21.0 nM 7.68
CHEMBL2113157 Ki = 24.0 nM 7.62
CHEMBL2113158 Ki = 31.0 nM 7.51
CHEMBL2113159 Ki = 37.0 nM 7.43
CHEMBL198226 Ki = 47.0 nM 7.33
CHEMBL408379 Ki = 50.0 nM 7.30
CHEMBL2113160 Ki = 113.0 nM 6.95
CHEMBL198372 Ki = 200.0 nM 6.70
CHEMBL198371 Ki = 488.0 nM 6.31