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Assay Detail

CHEMBL930537

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

Binding
Displacement of [3H]neomonapride from dopamine D2 receptor in rat striatum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and dopamine receptor affinities of N-alkyl-11-hydroxy-2-methoxynoraporphines: N-alkyl substituents determine D1 versus D2 receptor selectivity.
Si YG, Gardner MP, Tarazi FI, Baldessarini RJ, Neumeyer JL.
J Med Chem (2008) 51 : 983 -987
PubMed 18251489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.91 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 9.05
CHEMBL53294 1 8.89
CHEMBL53 APOMORPHINE 4.0 1 8.72
CHEMBL53445 1 8.46
CHEMBL405369 1 7.55
CHEMBL27559 1 7.54
CHEMBL405345 1 7.36
CHEMBL119455 1 6.97
CHEMBL270426 1 6.63
CHEMBL406269 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Ki = 0.9 nM 9.05
CHEMBL53294 Ki = 1.3 nM 8.89
CHEMBL53 APOMORPHINE Ki = 1.9 nM 8.72
CHEMBL53445 Ki = 3.5 nM 8.46
CHEMBL405369 Ki = 28.0 nM 7.55
CHEMBL27559 Ki = 28.5 nM 7.54
CHEMBL405345 Ki = 44.0 nM 7.36
CHEMBL119455 Ki = 108.0 nM 6.97
CHEMBL270426 Ki = 235.0 nM 6.63
CHEMBL406269 Ki > 10000.0 nM -