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Assay Detail

CHEMBL676130

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

Binding
In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 from rat brain limbic tissue
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Limbic system
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies.
Abou-Gharbia M, Patel UR, Webb MB, Moyer JA, Andree TH, Muth EA.
J Med Chem (1988) 31 : 1382 -1392
PubMed 2898533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.61 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1202507 1 7.80
CHEMBL1202512 1 7.28
CHEMBL28406 1 7.19
CHEMBL31319 1 7.13
CHEMBL1202513 1 7.07
CHEMBL49 BUSPIRONE 4.0 1 6.92
CHEMBL1202494 1 6.85
CHEMBL28352 1 6.61
CHEMBL1204094 1 6.46
CHEMBL412258 1 6.46
CHEMBL28453 1 6.43
CHEMBL284203 1 6.38
CHEMBL1202504 1 6.31
CHEMBL29155 1 6.16
CHEMBL281215 1 6.01
CHEMBL424409 1 5.72
CHEMBL29218 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1202507 Ki = 16.0 nM 7.80
CHEMBL1202512 Ki = 53.0 nM 7.28
CHEMBL28406 Ki = 65.0 nM 7.19
CHEMBL31319 Ki = 74.0 nM 7.13
CHEMBL1202513 Ki = 85.0 nM 7.07
CHEMBL49 BUSPIRONE Ki = 119.0 nM 6.92
CHEMBL1202494 Ki = 140.0 nM 6.85
CHEMBL28352 Ki = 248.0 nM 6.61
CHEMBL1204094 Ki = 345.0 nM 6.46
CHEMBL412258 Ki = 345.0 nM 6.46
CHEMBL28453 Ki = 374.0 nM 6.43
CHEMBL284203 Ki = 413.0 nM 6.38
CHEMBL1202504 Ki = 488.0 nM 6.31
CHEMBL29155 Ki = 690.0 nM 6.16
CHEMBL281215 Ki = 968.0 nM 6.01
CHEMBL424409 Ki = 1925.0 nM 5.72
CHEMBL29218 Ki = 2334.0 nM 5.63