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Assay Detail

CHEMBL676136

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

Binding
In vitro radioligand binding assay on Dopamine receptor D2 of rat striatum using [3H]- spiperone
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
Yasunaga T, Naito R, Kontani T, Tsukamoto S, Nomura T, Yamaguchi T, Mase T.
J Med Chem (1997) 40 : 1252 -1257
PubMed 9111299 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.17 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25213 1 9.59
CHEMBL22682 1 9.31
CHEMBL25215 1 9.24
CHEMBL25663 1 8.76
CHEMBL21475 1 8.75
CHEMBL22802 1 8.75
CHEMBL278806 1 8.45
CHEMBL22328 1 7.67
CHEMBL38288 1 6.75
CHEMBL22778 2 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25213 Ki = 0.259 nM 9.59
CHEMBL22682 Ki = 0.489 nM 9.31
CHEMBL25215 Ki = 0.581 nM 9.24
CHEMBL25663 Ki = 1.75 nM 8.76
CHEMBL21475 Ki = 1.79 nM 8.75
CHEMBL22802 Ki = 1.76 nM 8.75
CHEMBL278806 Ki = 3.53 nM 8.45
CHEMBL22328 Ki = 21.3 nM 7.67
CHEMBL38288 Ki = 176.0 nM 6.75
CHEMBL22778 Ki = 400.0 nM 6.40
CHEMBL22778 Ki = 614.0 nM 6.21