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Assay Detail

CHEMBL894057

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

Binding
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 7 (CHEMBL3223)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 15 7.17 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243954 1 9.89
CHEMBL18840 1 9.30
CHEMBL243955 1 9.05
CHEMBL243744 1 8.96
CHEMBL243523 1 8.15
CHEMBL244161 1 7.59
CHEMBL243742 1 7.30
CHEMBL244577 1 6.88
CHEMBL390213 1 6.56
CHEMBL389110 1 6.47
CHEMBL243953 1 6.27
CHEMBL243743 1 5.55
CHEMBL390015 1 5.37
CHEMBL244792 1 5.09
CHEMBL244162 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243954 Ki = 0.13 nM 9.89
CHEMBL18840 Ki = 0.5 nM 9.30
CHEMBL243955 Ki = 0.9 nM 9.05
CHEMBL243744 Ki = 1.1 nM 8.96
CHEMBL243523 Ki = 7.1 nM 8.15
CHEMBL244161 Ki = 25.4 nM 7.59
CHEMBL243742 Ki = 49.6 nM 7.30
CHEMBL244577 Ki = 131.0 nM 6.88
CHEMBL390213 Ki = 278.0 nM 6.56
CHEMBL389110 Ki = 338.0 nM 6.47
CHEMBL243953 Ki = 538.0 nM 6.27
CHEMBL243743 Ki = 2810.0 nM 5.55
CHEMBL390015 Ki = 4253.0 nM 5.37
CHEMBL244792 Ki = 8027.0 nM 5.09
CHEMBL244162 Ki = 8178.0 nM 5.09