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Assay Detail

CHEMBL919045

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in Wistar Han rat cortex membranes
20
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 18 6.18 7.11
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222188 1 7.11
CHEMBL224883 1 6.85
CHEMBL374297 1 6.59
CHEMBL222755 1 6.58
CHEMBL225571 1 6.55
CHEMBL222477 1 6.52
CHEMBL225284 1 6.49
CHEMBL221513 1 6.16
CHEMBL224935 1 6.04
CHEMBL374298 1 5.95
CHEMBL225512 1 5.47
CHEMBL374261 1 5.14
CHEMBL389718 1 4.91
CHEMBL222275 1 -
CHEMBL225171 1 -
CHEMBL222507 1 -
CHEMBL387738 2 -
CHEMBL222489 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222188 Ki = 77.8 nM 7.11
CHEMBL224883 Ki = 142.0 nM 6.85
CHEMBL374297 Ki = 259.0 nM 6.59
CHEMBL222755 Ki = 262.0 nM 6.58
CHEMBL225571 Ki = 282.0 nM 6.55
CHEMBL222477 Ki = 301.0 nM 6.52
CHEMBL225284 Ki = 326.0 nM 6.49
CHEMBL221513 Ki = 700.0 nM 6.16
CHEMBL224935 Ki = 909.0 nM 6.04
CHEMBL374298 Ki = 1127.0 nM 5.95
CHEMBL225512 Ki = 3394.0 nM 5.47
CHEMBL374261 Ki = 7168.0 nM 5.14
CHEMBL389718 Ki = 12200.0 nM 4.91
CHEMBL222275 Ki - -
CHEMBL225171 Ki - -
CHEMBL222507 Ki - -
CHEMBL387738 Activity = 38.0 % -
CHEMBL387738 Ki > 4000.0 nM -
CHEMBL222489 Activity = 9.0 % -
CHEMBL222489 Ki > 4000.0 nM -