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Assay Detail

CHEMBL619040

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

Binding
Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand
41
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 4 (CHEMBL4317)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
Yang D, Soulier JL, Sicsic S, Mathé-Allainmat M, Brémont B, Croci T, Cardamone R, Aureggi G, Langlois M.
J Med Chem (1997) 40 : 608 -621
PubMed 9046352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 7.99 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33884 1 9.82
CHEMBL155917 2 9.59
CHEMBL348311 1 9.04
CHEMBL156349 1 9.03
CHEMBL157880 3 9.00
CHEMBL156348 1 8.98
CHEMBL286136 1 8.97
CHEMBL347235 1 8.85
CHEMBL156554 1 8.85
CHEMBL155682 1 8.76
CHEMBL158238 1 8.39
CHEMBL156970 1 8.27
CHEMBL158147 1 8.26
CHEMBL287045 1 8.26
CHEMBL156088 1 8.22
CHEMBL155631 1 8.21
CHEMBL351570 1 8.20
CHEMBL160237 1 8.12
CHEMBL349809 1 8.11
CHEMBL156579 1 8.04
CHEMBL156965 1 8.03
CHEMBL83954 1 7.55
CHEMBL157631 1 7.45
CHEMBL157233 1 7.40
CHEMBL160705 1 7.33
CHEMBL301039 1 7.31
CHEMBL33676 1 7.19
CHEMBL288199 1 7.04
CHEMBL351557 1 6.99
CHEMBL420969 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33884 Ki = 0.15 nM 9.82
CHEMBL155917 Ki = 0.26 nM 9.59
CHEMBL348311 Ki = 0.92 nM 9.04
CHEMBL156349 Ki = 0.93 nM 9.03
CHEMBL157880 Ki = 1.0 nM 9.00
CHEMBL156348 Ki = 1.05 nM 8.98
CHEMBL286136 Ki = 1.07 nM 8.97
CHEMBL156554 Ki = 1.43 nM 8.85
CHEMBL347235 Ki = 1.42 nM 8.85
CHEMBL155682 Ki = 1.72 nM 8.76
CHEMBL157880 Ki = 2.0 nM 8.70
CHEMBL155917 Ki = 2.32 nM 8.63
CHEMBL158238 Ki = 4.08 nM 8.39
CHEMBL157880 Ki = 4.8 nM 8.32
CHEMBL156970 Ki = 5.35 nM 8.27
CHEMBL158147 Ki = 5.45 nM 8.26
CHEMBL287045 Ki = 5.5 nM 8.26
CHEMBL156088 Ki = 6.03 nM 8.22
CHEMBL155631 Ki = 6.2 nM 8.21
CHEMBL351570 Ki = 6.28 nM 8.20
CHEMBL160237 Ki = 7.64 nM 8.12
CHEMBL349809 Ki = 7.8 nM 8.11
CHEMBL156579 Ki = 9.1 nM 8.04
CHEMBL156965 Ki = 9.3 nM 8.03
CHEMBL83954 Ki = 28.1 nM 7.55
CHEMBL157631 Ki = 35.6 nM 7.45
CHEMBL157233 Ki = 39.5 nM 7.40
CHEMBL160705 Ki = 47.0 nM 7.33
CHEMBL301039 Ki = 48.6 nM 7.31
CHEMBL33676 Ki = 64.3 nM 7.19
CHEMBL288199 Ki = 91.4 nM 7.04
CHEMBL351557 Ki = 103.0 nM 6.99
CHEMBL420969 Ki = 135.0 nM 6.87
CHEMBL39 SEROTONIN Ki = 187.0 nM 6.73
CHEMBL59834 Ki = 257.0 nM 6.59
CHEMBL28992 Ki = 383.0 nM 6.42
CHEMBL41769 Ki = 488.0 nM 6.31
CHEMBL27846 (R)ZACOPRIDE Ki = 1510.0 nM 5.82
CHEMBL86 METOCLOPRAMIDE Ki > 1000.0 nM -
CHEMBL76737 Ki > 1000.0 nM -
CHEMBL156499 Ki > 1000.0 nM -