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Assay Detail

CHEMBL872888

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

Binding
In vitro binding affinity for dopamine receptor D2 on rat striatal membranes by [3H]spiperone displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

3-[[(4-Aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as dopamine D2 partial agonists and autoreceptor agonists.
Wustrow DJ, Smith WJ, Corbin AE, Davis MD, Georgic LM, Pugsley TA, Whetzel SZ, Heffner TG, Wise LD.
J Med Chem (1997) 40 : 250 -259
PubMed 9003524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.96 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313095 1 8.07
CHEMBL86662 1 8.06
CHEMBL431367 ROXINDOLE 2.0 1 7.85
CHEMBL87003 1 7.55
CHEMBL554027 1 7.54
CHEMBL423499 1 7.30
CHEMBL314987 1 7.08
CHEMBL87504 1 7.07
CHEMBL85018 1 6.96
CHEMBL84851 1 6.91
CHEMBL314888 1 6.91
CHEMBL86801 1 6.86
CHEMBL87924 1 6.79
CHEMBL87481 1 6.57
CHEMBL418937 1 6.38
CHEMBL86517 1 6.34
CHEMBL86887 1 6.20
CHEMBL315655 1 6.19
CHEMBL90673 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313095 Ki = 8.6 nM 8.07
CHEMBL86662 Ki = 8.7 nM 8.06
CHEMBL431367 ROXINDOLE Ki = 14.0 nM 7.85
CHEMBL87003 Ki = 28.0 nM 7.55
CHEMBL554027 Ki = 29.0 nM 7.54
CHEMBL423499 Ki = 50.0 nM 7.30
CHEMBL314987 Ki = 83.0 nM 7.08
CHEMBL87504 Ki = 85.0 nM 7.07
CHEMBL85018 Ki = 110.0 nM 6.96
CHEMBL84851 Ki = 122.0 nM 6.91
CHEMBL314888 Ki = 124.0 nM 6.91
CHEMBL86801 Ki = 139.0 nM 6.86
CHEMBL87924 Ki = 161.0 nM 6.79
CHEMBL87481 Ki = 270.0 nM 6.57
CHEMBL418937 Ki = 412.0 nM 6.38
CHEMBL86517 Ki = 457.0 nM 6.34
CHEMBL86887 Ki = 630.0 nM 6.20
CHEMBL315655 Ki = 645.0 nM 6.19
CHEMBL90673 Ki = 2596.0 nM 5.59