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Assay Detail

CHEMBL675662

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

Binding
Binding affinity at rat striatal Dopamine receptor D2 using [3H]- piperone radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues.
Gao YG, Baldessarini RJ, Kula NS, Neumeyer JL.
J Med Chem (1990) 33 : 1800 -1805
PubMed 1971309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.42 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288096 1 10.28
CHEMBL53294 1 9.77
CHEMBL19130 1 9.42
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 9.10
CHEMBL53445 1 8.95
CHEMBL53 APOMORPHINE 4.0 1 7.96
CHEMBL276326 1 7.75
CHEMBL431946 1 7.65
CHEMBL301761 1 7.46
CHEMBL416288 (S)APOMORPHINE 1 7.23
CHEMBL54183 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288096 Ki = 0.053 nM 10.28
CHEMBL53294 Ki = 0.17 nM 9.77
CHEMBL19130 Ki = 0.38 nM 9.42
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Ki = 0.8 nM 9.10
CHEMBL53445 Ki = 1.12 nM 8.95
CHEMBL53 APOMORPHINE Ki = 11.1 nM 7.96
CHEMBL276326 Ki = 17.7 nM 7.75
CHEMBL431946 Ki = 22.3 nM 7.65
CHEMBL301761 Ki = 34.7 nM 7.46
CHEMBL416288 (S)APOMORPHINE Ki = 58.3 nM 7.23
CHEMBL54183 Ki = 100.0 nM 7.00