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Assay Detail

CHEMBL830441

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

Binding
Displacement of [3H]granisetron from 5-hydroxytryptamine 3 receptor of rat cortical membrane
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.
Cappelli A, Gallelli A, Manini M, Anzini M, Mennuni L, Makovec F, Menziani MC, Alcaro S, Ortuso F, Vomero S.
J Med Chem (2005) 48 : 3564 -3575
PubMed 15887964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 8.89 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439857 1 10.10
CHEMBL191035 1 9.96
CHEMBL195881 1 9.77
CHEMBL192675 1 9.68
CHEMBL43355 1 9.64
CHEMBL64078 1 9.62
CHEMBL289469 GRANISETRON 4.0 1 9.46
CHEMBL364501 1 9.43
CHEMBL191036 1 9.39
CHEMBL372262 1 9.37
CHEMBL191900 1 9.35
CHEMBL363595 1 9.29
CHEMBL191084 1 9.26
CHEMBL371144 1 9.25
CHEMBL192869 1 9.17
CHEMBL192220 1 9.11
CHEMBL192794 1 9.08
CHEMBL192930 1 9.07
CHEMBL193318 1 9.04
CHEMBL194492 1 8.96
CHEMBL195056 1 8.92
CHEMBL195498 1 8.80
CHEMBL193460 1 8.80
CHEMBL191649 1 8.68
CHEMBL192611 1 8.66
CHEMBL195490 1 8.62
CHEMBL364895 1 8.57
CHEMBL191707 1 8.52
CHEMBL195902 1 8.44
CHEMBL364957 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439857 Ki = 0.08 nM 10.10
CHEMBL191035 Ki = 0.11 nM 9.96
CHEMBL195881 Ki = 0.17 nM 9.77
CHEMBL192675 Ki = 0.21 nM 9.68
CHEMBL43355 Ki = 0.23 nM 9.64
CHEMBL64078 Ki = 0.24 nM 9.62
CHEMBL289469 GRANISETRON Ki = 0.35 nM 9.46
CHEMBL364501 Ki = 0.37 nM 9.43
CHEMBL191036 Ki = 0.41 nM 9.39
CHEMBL372262 Ki = 0.43 nM 9.37
CHEMBL191900 Ki = 0.45 nM 9.35
CHEMBL363595 Ki = 0.51 nM 9.29
CHEMBL191084 Ki = 0.55 nM 9.26
CHEMBL371144 Ki = 0.56 nM 9.25
CHEMBL192869 Ki = 0.68 nM 9.17
CHEMBL192220 Ki = 0.78 nM 9.11
CHEMBL192794 Ki = 0.84 nM 9.08
CHEMBL192930 Ki = 0.85 nM 9.07
CHEMBL193318 Ki = 0.92 nM 9.04
CHEMBL194492 Ki = 1.1 nM 8.96
CHEMBL195056 Ki = 1.2 nM 8.92
CHEMBL195498 Ki = 1.6 nM 8.80
CHEMBL193460 Ki = 1.6 nM 8.80
CHEMBL191649 Ki = 2.1 nM 8.68
CHEMBL192611 Ki = 2.2 nM 8.66
CHEMBL195490 Ki = 2.4 nM 8.62
CHEMBL364895 Ki = 2.7 nM 8.57
CHEMBL191707 Ki = 3.0 nM 8.52
CHEMBL195902 Ki = 3.6 nM 8.44
CHEMBL364957 Ki = 4.2 nM 8.38
CHEMBL195241 Ki = 5.6 nM 8.25
CHEMBL192350 Ki = 6.2 nM 8.21
CHEMBL372203 Ki = 10.0 nM 8.00
CHEMBL191458 Ki = 13.0 nM 7.89
CHEMBL365180 Ki = 14.0 nM 7.85
CHEMBL436287 Ki = 19.0 nM 7.72
CHEMBL191763 Ki = 188.0 nM 6.73