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Assay Detail

CHEMBL894061

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

Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
15
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 7 (CHEMBL5494)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R.
J Med Chem (2007) 50 : 4214 -4221
PubMed 17649988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
%max 8 - -
EC50 7 5.54 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18840 2 6.20
CHEMBL243744 2 6.05
CHEMBL243955 2 5.93
CHEMBL243954 2 5.75
CHEMBL222188 2 5.10
CHEMBL225571 2 5.00
CHEMBL222477 2 4.77
CHEMBL244161 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18840 EC50 = 630.0 nM 6.20
CHEMBL243744 EC50 = 900.0 nM 6.05
CHEMBL243955 EC50 = 1170.0 nM 5.93
CHEMBL243954 EC50 = 1770.0 nM 5.75
CHEMBL222188 EC50 = 8000.0 nM 5.10
CHEMBL225571 EC50 = 10000.0 nM 5.00
CHEMBL222477 EC50 = 17000.0 nM 4.77
CHEMBL18840 %max = 100.0 % -
CHEMBL244161 %max = - % -
CHEMBL243955 %max = 100.0 % -
CHEMBL243954 %max = 74.0 % -
CHEMBL243744 %max = 83.0 % -
CHEMBL222477 %max = 13.0 % -
CHEMBL225571 %max = 24.0 % -
CHEMBL222188 %max = 40.0 % -