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Assay Detail

CHEMBL616692

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

Binding
Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampus mambranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
Orjales A, Mosquera R, Toledo A, Pumar MC, García N, Cortizo L, Labeaga L, Innerárity A.
J Med Chem (2003) 46 : 5512 -5532
PubMed 14640559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.16 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.92
CHEMBL151043 1 7.47
CHEMBL356250 1 7.42
CHEMBL346203 1 7.16
CHEMBL152997 1 7.15
CHEMBL421787 1 7.03
CHEMBL423034 1 6.97
CHEMBL357308 1 6.93
CHEMBL153685 1 6.74
CHEMBL153684 1 6.59
CHEMBL150333 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 1.2 nM 8.92
CHEMBL151043 Ki = 33.7 nM 7.47
CHEMBL356250 Ki = 37.8 nM 7.42
CHEMBL346203 Ki = 69.7 nM 7.16
CHEMBL152997 Ki = 70.2 nM 7.15
CHEMBL421787 Ki = 93.6 nM 7.03
CHEMBL423034 Ki = 107.8 nM 6.97
CHEMBL357308 Ki = 117.7 nM 6.93
CHEMBL153685 Ki = 182.0 nM 6.74
CHEMBL153684 Ki = 254.3 nM 6.59
CHEMBL150333 Ki = 445.6 nM 6.35