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Assay Detail

CHEMBL2090846

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

Binding
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
Del Bello F, Diamanti E, Giannella M, Mammoli V, Marchioro C, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Benedetti G, Varrone M, Pigini M.
ACS Med Chem Lett (2012) 3 : 535 -539
PubMed 24900506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.44 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.47
CHEMBL2089156 1 8.24
CHEMBL1956195 CYCLOMETHYLINE 1 7.98
CHEMBL495095 ALLYPHENYLINE 1 7.55
CHEMBL1276140 1 7.45
CHEMBL2089155 1 7.40
CHEMBL17860 LOFEXIDINE 4.0 1 6.90
CHEMBL134 CLONIDINE 4.0 1 5.49
CHEMBL1276139 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 3.388 nM 8.47
CHEMBL2089156 Ki = 5.754 nM 8.24
CHEMBL1956195 CYCLOMETHYLINE Ki = 10.47 nM 7.98
CHEMBL495095 ALLYPHENYLINE Ki = 28.18 nM 7.55
CHEMBL1276140 Ki = 35.48 nM 7.45
CHEMBL2089155 Ki = 39.81 nM 7.40
CHEMBL17860 LOFEXIDINE Ki = 125.89 nM 6.90
CHEMBL134 CLONIDINE Ki = 3235.94 nM 5.49
CHEMBL1276139 Ki > 10000.0 nM -