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Assay Detail

CHEMBL616595

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

Binding
Binding affinities against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in rat cerebral cortex membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
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. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity.
López-Rodríguez ML, Morcillo MJ, Fernández E, Porras E, Murcia M, Sanz AM, Orensanz L.
J Med Chem (1997) 40 : 2653 -2656
PubMed 9258372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.02 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46918 1 8.62
CHEMBL42706 1 8.42
CHEMBL43992 1 8.39
CHEMBL289873 1 8.36
CHEMBL88715 1 8.29
CHEMBL42810 1 8.26
CHEMBL45253 1 8.24
CHEMBL42644 1 8.14
CHEMBL46881 1 8.06
CHEMBL417709 1 8.00
CHEMBL290039 1 7.95
CHEMBL90165 1 7.91
CHEMBL88594 1 7.91
CHEMBL89380 1 7.86
CHEMBL90384 1 7.82
CHEMBL315472 1 7.76
CHEMBL314997 1 7.61
CHEMBL89677 1 7.61
CHEMBL424432 1 7.55
CHEMBL89950 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46918 Ki = 2.4 nM 8.62
CHEMBL42706 Ki = 3.8 nM 8.42
CHEMBL43992 Ki = 4.1 nM 8.39
CHEMBL289873 Ki = 4.4 nM 8.36
CHEMBL88715 Ki = 5.1 nM 8.29
CHEMBL42810 Ki = 5.5 nM 8.26
CHEMBL45253 Ki = 5.7 nM 8.24
CHEMBL42644 Ki = 7.2 nM 8.14
CHEMBL46881 Ki = 8.8 nM 8.06
CHEMBL417709 Ki = 9.9 nM 8.00
CHEMBL290039 Ki = 11.3 nM 7.95
CHEMBL90165 Ki = 12.3 nM 7.91
CHEMBL88594 Ki = 12.2 nM 7.91
CHEMBL89380 Ki = 13.9 nM 7.86
CHEMBL90384 Ki = 15.3 nM 7.82
CHEMBL315472 Ki = 17.5 nM 7.76
CHEMBL314997 Ki = 24.3 nM 7.61
CHEMBL89677 Ki = 24.3 nM 7.61
CHEMBL424432 Ki = 28.1 nM 7.55
CHEMBL89950 Ki = 29.1 nM 7.54