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Assay Detail

CHEMBL615460

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

Binding
Tested in vitro for the inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor, expressed in cloned CHO cells.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists
Stjernlof P, Lin C, Sonesson C, Svensson K, Smith MW
Bioorg Med Chem Lett (1997) 7 : 2759 -2764
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.80 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430332 1 9.70
CHEMBL56 8-OH-DPAT 1 9.40
CHEMBL328107 1 8.41
CHEMBL93186 1 8.21
CHEMBL314548 1 8.11
CHEMBL285755 1 7.33
CHEMBL433002 1 6.92
CHEMBL278751 1 6.78
CHEMBL96735 1 6.68
CHEMBL273273 5-OH-DPAT 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430332 Ki = 0.2 nM 9.70
CHEMBL56 8-OH-DPAT Ki = 0.4 nM 9.40
CHEMBL328107 Ki = 3.9 nM 8.41
CHEMBL93186 Ki = 6.1 nM 8.21
CHEMBL314548 Ki = 7.8 nM 8.11
CHEMBL285755 Ki = 47.0 nM 7.33
CHEMBL433002 Ki = 120.0 nM 6.92
CHEMBL278751 Ki = 168.0 nM 6.78
CHEMBL96735 Ki = 210.0 nM 6.68
CHEMBL273273 5-OH-DPAT Ki = 344.0 nM 6.46