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Assay Detail

CHEMBL1063142

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

Binding
Displacement of [3H]raclopride from rat dopamine D2short receptor expressed in CHO-K1 cells by liquid scintillation counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists.
Herm L, Berényi S, Vonk A, Rinken A, Sipos A.
Bioorg Med Chem (2009) 17 : 4756 -4762
PubMed 19454369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.79 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL562935 1 8.82
CHEMBL560721 1 8.70
CHEMBL517028 1 8.38
CHEMBL550180 1 8.04
CHEMBL53 APOMORPHINE 4.0 1 7.94
CHEMBL465054 1 7.93
CHEMBL564909 1 7.85
CHEMBL557547 1 7.68
CHEMBL562460 1 6.94
CHEMBL550792 1 6.72
CHEMBL59 DOPAMINE 4.0 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL562935 Ki = 1.5 nM 8.82
CHEMBL560721 Ki = 2.0 nM 8.70
CHEMBL517028 Ki = 4.14 nM 8.38
CHEMBL550180 Ki = 9.2 nM 8.04
CHEMBL53 APOMORPHINE Ki = 11.5 nM 7.94
CHEMBL465054 Ki = 11.7 nM 7.93
CHEMBL564909 Ki = 14.0 nM 7.85
CHEMBL557547 Ki = 20.7 nM 7.68
CHEMBL562460 Ki = 115.0 nM 6.94
CHEMBL550792 Ki = 192.0 nM 6.72
CHEMBL59 DOPAMINE Ki = 197.0 nM 6.71