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Assay Detail

CHEMBL620632

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

Binding
Binding affinity for 5-hydroxytryptamine 3 receptor from rat cortex using [3H]BRL-43694 as radioligand
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
Anzini M, Cappelli A, Vomero S, Giorgi G, Langer T, Hamon M, Merahi N, Emerit BM, Cagnotto A, Skorupska M.
J Med Chem (1995) 38 : 2692 -2704
PubMed 7629808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.75 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18772 QUIPAZINE 2.0 1 8.92
CHEMBL46 ONDANSETRON 4.0 1 8.92
CHEMBL304193 1 8.80
CHEMBL417706 1 8.46
CHEMBL62589 1 8.42
CHEMBL62636 1 8.27
CHEMBL64416 1 8.10
CHEMBL41462 1 8.02
CHEMBL64879 1 7.94
CHEMBL59871 1 7.91
CHEMBL293866 1 7.90
CHEMBL293703 1 7.84
CHEMBL292260 1 7.79
CHEMBL430566 1 7.49
CHEMBL291771 1 7.38
CHEMBL304016 1 7.34
CHEMBL64146 1 7.28
CHEMBL62449 1 7.27
CHEMBL303999 1 7.18
CHEMBL39 SEROTONIN 3.0 1 7.18
CHEMBL61007 1 6.89
CHEMBL293218 1 6.66
CHEMBL64145 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18772 QUIPAZINE Ki = 1.2 nM 8.92
CHEMBL46 ONDANSETRON Ki = 1.2 nM 8.92
CHEMBL304193 Ki = 1.6 nM 8.80
CHEMBL417706 Ki = 3.5 nM 8.46
CHEMBL62589 Ki = 3.8 nM 8.42
CHEMBL62636 Ki = 5.4 nM 8.27
CHEMBL64416 Ki = 8.0 nM 8.10
CHEMBL41462 Ki = 9.5 nM 8.02
CHEMBL64879 Ki = 11.5 nM 7.94
CHEMBL59871 Ki = 12.3 nM 7.91
CHEMBL293866 Ki = 12.5 nM 7.90
CHEMBL293703 Ki = 14.4 nM 7.84
CHEMBL292260 Ki = 16.4 nM 7.79
CHEMBL430566 Ki = 32.5 nM 7.49
CHEMBL291771 Ki = 41.6 nM 7.38
CHEMBL304016 Ki = 45.9 nM 7.34
CHEMBL64146 Ki = 52.2 nM 7.28
CHEMBL62449 Ki = 53.3 nM 7.27
CHEMBL303999 Ki = 66.5 nM 7.18
CHEMBL39 SEROTONIN Ki = 66.0 nM 7.18
CHEMBL61007 Ki = 130.0 nM 6.89
CHEMBL293218 Ki = 220.0 nM 6.66
CHEMBL64145 Ki = 410.0 nM 6.39