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Assay Detail

CHEMBL644243

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

Binding
Binding affinities against Alpha-1 adrenergic receptor (alpha1 adrenoceptor) using [3H]prazosin 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

Alpha-1A adrenergic receptor (CHEMBL319)
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 7.28 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289873 1 8.51
CHEMBL42810 1 8.08
CHEMBL46881 1 8.07
CHEMBL290039 1 8.02
CHEMBL43992 1 8.00
CHEMBL42644 1 7.92
CHEMBL88715 1 7.35
CHEMBL89677 1 7.19
CHEMBL424432 1 7.19
CHEMBL46918 1 7.19
CHEMBL315472 1 7.14
CHEMBL417709 1 7.14
CHEMBL45253 1 7.04
CHEMBL42706 1 6.96
CHEMBL90384 1 6.94
CHEMBL89380 1 6.66
CHEMBL90165 1 6.62
CHEMBL314997 1 6.56
CHEMBL88594 1 6.49
CHEMBL89950 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289873 Ki = 3.1 nM 8.51
CHEMBL42810 Ki = 8.3 nM 8.08
CHEMBL46881 Ki = 8.6 nM 8.07
CHEMBL290039 Ki = 9.6 nM 8.02
CHEMBL43992 Ki = 9.9 nM 8.00
CHEMBL42644 Ki = 12.1 nM 7.92
CHEMBL88715 Ki = 45.0 nM 7.35
CHEMBL89677 Ki = 64.3 nM 7.19
CHEMBL424432 Ki = 64.9 nM 7.19
CHEMBL46918 Ki = 64.9 nM 7.19
CHEMBL315472 Ki = 72.6 nM 7.14
CHEMBL417709 Ki = 72.4 nM 7.14
CHEMBL45253 Ki = 90.4 nM 7.04
CHEMBL42706 Ki = 109.0 nM 6.96
CHEMBL90384 Ki = 115.0 nM 6.94
CHEMBL89380 Ki = 218.0 nM 6.66
CHEMBL90165 Ki = 240.0 nM 6.62
CHEMBL314997 Ki = 278.0 nM 6.56
CHEMBL88594 Ki = 323.0 nM 6.49
CHEMBL89950 Ki = 363.0 nM 6.44