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Assay Detail

CHEMBL830403

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

Binding
Binding affinity for D2-like [3H]spiperone receptor was determined using caudate-putamen of adult male Spragueo?=Dawley rats
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Caudate-putamen
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands.
Ji M, Chen J, Ding K, Ding K, Wu X, Varady J, Levant B, Wang S.
Bioorg Med Chem Lett (2005) 15 : 1701 -1705
PubMed 15745825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.07 6.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25236 BP-897 1 6.79
CHEMBL426425 1 6.66
CHEMBL341774 1 6.61
CHEMBL362665 1 6.59
CHEMBL359654 1 6.12
CHEMBL179376 1 6.07
CHEMBL181203 1 6.04
CHEMBL179781 1 5.95
CHEMBL179805 1 5.86
CHEMBL179757 1 5.80
CHEMBL180107 1 5.61
CHEMBL345106 1 5.44
CHEMBL413554 1 5.41
CHEMBL368686 1 -
CHEMBL361756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25236 BP-897 Ki = 162.0 nM 6.79
CHEMBL426425 Ki = 220.0 nM 6.66
CHEMBL341774 Ki = 243.0 nM 6.61
CHEMBL362665 Ki = 258.0 nM 6.59
CHEMBL359654 Ki = 762.0 nM 6.12
CHEMBL179376 Ki = 852.0 nM 6.07
CHEMBL181203 Ki = 906.0 nM 6.04
CHEMBL179781 Ki = 1125.0 nM 5.95
CHEMBL179805 Ki = 1389.0 nM 5.86
CHEMBL179757 Ki = 1568.0 nM 5.80
CHEMBL180107 Ki = 2443.0 nM 5.61
CHEMBL345106 Ki = 3643.0 nM 5.44
CHEMBL413554 Ki = 3887.0 nM 5.41
CHEMBL368686 Ki > 100.0 nM -
CHEMBL361756 Ki > 250000.0 nM -