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Assay Detail

CHEMBL615968

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Binding
In vitro binding affinity against 5-hydroxytryptamine 1A receptor of rat cerebral cortex using [3H]8-OH-DPAT as radioligand.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous 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. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparison of CoMFA models.
López-Rodríguez ML, Rosado ML, Benhamú B, Morcillo MJ, Fernández E, Schaper KJ.
J Med Chem (1997) 40 : 1648 -1656
PubMed 9171874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.72 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL295168 1 7.51
CHEMBL46471 1 7.46
CHEMBL297844 1 7.24
CHEMBL297887 1 7.23
CHEMBL295244 1 7.11
CHEMBL46470 1 7.07
CHEMBL42654 1 7.00
CHEMBL430567 1 6.92
CHEMBL46672 1 6.35
CHEMBL42881 1 6.30
CHEMBL46862 1 5.22
CHEMBL295527 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL295168 Ki = 31.1 nM 7.51
CHEMBL46471 Ki = 34.9 nM 7.46
CHEMBL297844 Ki = 57.7 nM 7.24
CHEMBL297887 Ki = 58.4 nM 7.23
CHEMBL295244 Ki = 78.6 nM 7.11
CHEMBL46470 Ki = 85.3 nM 7.07
CHEMBL42654 Ki = 101.0 nM 7.00
CHEMBL430567 Ki = 120.0 nM 6.92
CHEMBL46672 Ki = 444.0 nM 6.35
CHEMBL42881 Ki = 500.0 nM 6.30
CHEMBL46862 Ki = 5970.0 nM 5.22
CHEMBL295527 Ki = 6095.0 nM 5.21