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Assay Detail

CHEMBL617763

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

Binding
Compound was tested for binding affinity against human 5-hydroxytryptamine 2C receptor
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD.
J Med Chem (1998) 41 : 1218 -1235
PubMed 9548813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.20 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281350 SB-224289 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281350 SB-224289 Ki = 630.96 nM 6.20