Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL839644

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

Binding
In vitro inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.
López-Rodríguez ML, Morcillo MJ, Fernández E, Benhamú B, Tejada I, Ayala D, Viso A, Campillo M, Pardo L, Delgado M, Manzanares J, Fuentes JA.
J Med Chem (2005) 48 : 2548 -2558
PubMed 15801844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.27 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192512 1 9.30
CHEMBL421130 1 8.92
CHEMBL33150 1 8.62
CHEMBL370518 1 8.60
CHEMBL34288 1 8.51
CHEMBL370758 1 8.39
CHEMBL33258 1 8.39
CHEMBL366206 1 8.38
CHEMBL427349 1 8.34
CHEMBL445055 1 8.25
CHEMBL2113057 1 8.21
CHEMBL192875 1 8.20
CHEMBL426639 1 8.19
CHEMBL285066 1 8.17
CHEMBL34287 1 8.03
CHEMBL364241 1 8.02
CHEMBL430914 1 7.98
CHEMBL372014 1 7.94
CHEMBL192750 1 7.91
CHEMBL190284 1 7.82
CHEMBL416266 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192512 Ki = 0.5 nM 9.30
CHEMBL421130 Ki = 1.2 nM 8.92
CHEMBL33150 Ki = 2.4 nM 8.62
CHEMBL370518 Ki = 2.5 nM 8.60
CHEMBL34288 Ki = 3.1 nM 8.51
CHEMBL370758 Ki = 4.1 nM 8.39
CHEMBL33258 Ki = 4.1 nM 8.39
CHEMBL366206 Ki = 4.2 nM 8.38
CHEMBL427349 Ki = 4.6 nM 8.34
CHEMBL445055 Ki = 5.6 nM 8.25
CHEMBL2113057 Ki = 6.1 nM 8.21
CHEMBL192875 Ki = 6.3 nM 8.20
CHEMBL426639 Ki = 6.4 nM 8.19
CHEMBL285066 Ki = 6.7 nM 8.17
CHEMBL34287 Ki = 9.3 nM 8.03
CHEMBL364241 Ki = 9.5 nM 8.02
CHEMBL430914 Ki = 10.4 nM 7.98
CHEMBL372014 Ki = 11.6 nM 7.94
CHEMBL192750 Ki = 12.3 nM 7.91
CHEMBL190284 Ki = 15.3 nM 7.82
CHEMBL416266 Ki = 27.0 nM 7.57