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Assay Detail

CHEMBL619425

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

Binding
Binding affinity at 5-hydroxytryptamine 3 receptor in rat cortical membrane by [3H]graniestron displacement.
17
Total Activities
17
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 central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
Cappelli A, Anzini M, Vomero S, Mennuni L, Makovec F, Doucet E, Hamon M, Bruni G, Romeo MR, Menziani MC, De Benedetti PG, Langer T.
J Med Chem (1998) 41 : 728 -741
PubMed 9513601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.62 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43355 1 9.64
CHEMBL287987 1 9.08
CHEMBL18772 QUIPAZINE 2.0 1 8.74
CHEMBL43193 1 8.72
CHEMBL288591 1 8.52
CHEMBL352107 1 7.85
CHEMBL337213 1 7.42
CHEMBL336522 1 7.32
CHEMBL163440 1 7.23
CHEMBL126350 1 7.09
CHEMBL163279 1 6.96
CHEMBL351752 1 6.70
CHEMBL349542 1 6.70
CHEMBL162437 1 6.18
CHEMBL165721 1 6.08
CHEMBL166214 1 -
CHEMBL162219 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43355 Ki = 0.2291 nM 9.64
CHEMBL287987 Ki = 0.8318 nM 9.08
CHEMBL18772 QUIPAZINE Ki = 1.82 nM 8.74
CHEMBL43193 Ki = 1.905 nM 8.72
CHEMBL288591 Ki = 3.02 nM 8.52
CHEMBL352107 Ki = 14.13 nM 7.85
CHEMBL337213 Ki = 38.02 nM 7.42
CHEMBL336522 Ki = 47.86 nM 7.32
CHEMBL163440 Ki = 58.88 nM 7.23
CHEMBL126350 Ki = 81.28 nM 7.09
CHEMBL163279 Ki = 109.65 nM 6.96
CHEMBL351752 Ki = 199.53 nM 6.70
CHEMBL349542 Ki = 199.53 nM 6.70
CHEMBL162437 Ki = 660.69 nM 6.18
CHEMBL165721 Ki = 831.76 nM 6.08
CHEMBL166214 Ki < 549.54 nM -
CHEMBL162219 Ki < 549.54 nM -