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Assay Detail

CHEMBL919613

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Wistar Han rat hippocampal membranes
40
Total Activities
40
Compounds Tested
1
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 1A (CHEMBL273)
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 40 6.96 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.92
CHEMBL389718 1 8.42
CHEMBL224820 1 8.07
CHEMBL222864 1 8.05
CHEMBL221513 1 7.78
CHEMBL426723 1 7.63
CHEMBL225512 1 7.62
CHEMBL390558 1 7.61
CHEMBL222262 1 7.52
CHEMBL221732 1 7.41
CHEMBL225284 1 7.28
CHEMBL225252 1 7.26
CHEMBL449089 1 7.26
CHEMBL225441 1 7.14
CHEMBL376531 1 7.10
CHEMBL222477 1 7.02
CHEMBL224883 1 6.98
CHEMBL222188 1 6.89
CHEMBL390062 1 6.80
CHEMBL225571 1 6.74
CHEMBL222807 1 6.61
CHEMBL222106 1 6.60
CHEMBL28063 1 6.60
CHEMBL221453 1 6.59
CHEMBL376662 1 6.59
CHEMBL222755 1 6.55
CHEMBL224935 1 6.54
CHEMBL374261 1 6.48
CHEMBL224929 1 6.36
CHEMBL222489 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 1.2 nM 8.92
CHEMBL389718 Ki = 3.8 nM 8.42
CHEMBL224820 Ki = 8.6 nM 8.07
CHEMBL222864 Ki = 9.0 nM 8.05
CHEMBL221513 Ki = 16.6 nM 7.78
CHEMBL426723 Ki = 23.2 nM 7.63
CHEMBL225512 Ki = 24.0 nM 7.62
CHEMBL390558 Ki = 24.5 nM 7.61
CHEMBL222262 Ki = 30.0 nM 7.52
CHEMBL221732 Ki = 39.0 nM 7.41
CHEMBL225284 Ki = 52.7 nM 7.28
CHEMBL225252 Ki = 54.4 nM 7.26
CHEMBL449089 Ki = 55.0 nM 7.26
CHEMBL225441 Ki = 72.0 nM 7.14
CHEMBL376531 Ki = 78.9 nM 7.10
CHEMBL222477 Ki = 96.0 nM 7.02
CHEMBL224883 Ki = 105.0 nM 6.98
CHEMBL222188 Ki = 128.0 nM 6.89
CHEMBL390062 Ki = 160.0 nM 6.80
CHEMBL225571 Ki = 183.0 nM 6.74
CHEMBL222807 Ki = 245.0 nM 6.61
CHEMBL28063 Ki = 253.0 nM 6.60
CHEMBL222106 Ki = 253.0 nM 6.60
CHEMBL221453 Ki = 257.0 nM 6.59
CHEMBL376662 Ki = 254.0 nM 6.59
CHEMBL222755 Ki = 279.0 nM 6.55
CHEMBL224935 Ki = 291.0 nM 6.54
CHEMBL374261 Ki = 332.0 nM 6.48
CHEMBL224929 Ki = 441.0 nM 6.36
CHEMBL222489 Ki = 494.0 nM 6.31
CHEMBL374298 Ki = 676.0 nM 6.17
CHEMBL374297 Ki = 911.0 nM 6.04
CHEMBL388970 Ki = 2600.0 nM 5.58
CHEMBL387738 Ki = 3124.0 nM 5.50
CHEMBL222603 Ki = 3900.0 nM 5.41
CHEMBL222604 Ki - -
CHEMBL441560 Ki - -
CHEMBL222507 Ki - -
CHEMBL225171 Ki - -
CHEMBL222275 Ki - -