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Assay Detail

CHEMBL919048

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

Binding
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Niso M, Perrone R, Tortorella V.
J Med Chem (2004) 47 : 6616 -6624
PubMed 15588097 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 7.63 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224820 1 8.02
CHEMBL222755 1 7.80
CHEMBL225284 1 7.70
CHEMBL389718 1 7.60
CHEMBL18840 1 7.48
CHEMBL225512 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224820 Kd = 9.55 nM 8.02
CHEMBL222755 Kd = 15.85 nM 7.80
CHEMBL225284 Kd = 19.95 nM 7.70
CHEMBL389718 Kd = 25.12 nM 7.60
CHEMBL18840 Kd = 33.11 nM 7.48
CHEMBL225512 Kd = 63.1 nM 7.20