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Assay Detail

CHEMBL675759

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

Binding
Inhibition of [3H]N-propylnorapomorphine binding to Dopamine receptor D2 of rat striatal membranes
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.
Jaen JC, Wise LD, Caprathe BW, Tecle H, Bergmeier S, Humblet CC, Heffner TG, Meltzer LT, Pugsley TA.
J Med Chem (1990) 33 : 311 -317
PubMed 1967314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.90 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276500 2 6.74
CHEMBL106257 1 6.59
CHEMBL106028 1 6.39
CHEMBL93428 1 6.22
CHEMBL1203001 1 6.04
CHEMBL1203007 1 5.40
CHEMBL1203004 1 5.29
CHEMBL1203003 1 5.27
CHEMBL1202201 1 5.19
CHEMBL1203002 1 5.00
CHEMBL108682 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276500 IC50 = 183.0 nM 6.74
CHEMBL276500 IC50 = 184.0 nM 6.74
CHEMBL106257 IC50 = 257.0 nM 6.59
CHEMBL106028 IC50 = 411.0 nM 6.39
CHEMBL93428 IC50 = 596.0 nM 6.22
CHEMBL1203001 IC50 = 911.0 nM 6.04
CHEMBL1203007 IC50 = 3985.0 nM 5.40
CHEMBL1203004 IC50 = 5132.0 nM 5.29
CHEMBL1203003 IC50 = 5328.0 nM 5.27
CHEMBL1202201 IC50 = 6396.0 nM 5.19
CHEMBL1203002 IC50 = 10000.0 nM 5.00
CHEMBL108682 IC50 > 1000.0 nM -