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Assay Detail

CHEMBL884268

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

Binding
Inhibition of [3H]apomorphine binding to calf caudate membrane preparation (p4)
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Aporphines, 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal adenylate cyclase stimulation of 2,10,11-trihydroxyaporphines in comparison with other hydroxylated aporphines.
Neumeyer JL, Arana GW, Law SJ, Lamont JS, Kula NS, Baldessarini RJ.
J Med Chem (1981) 24 : 1440 -1445
PubMed 7310821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.37 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 9.00
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 2 8.60
CHEMBL19130 1 8.00
CHEMBL35556 1 7.62
CHEMBL285414 1 7.60
CHEMBL288096 1 7.60
CHEMBL286787 1 7.60
CHEMBL284248 1 7.52
CHEMBL27559 1 7.44
CHEMBL36061 1 6.95
CHEMBL32330 1 6.84
CHEMBL286929 1 6.69
CHEMBL283871 1 6.41
CHEMBL440846 1 6.16
CHEMBL154709 APOCIDEINE 1 5.62
CHEMBL284368 1 -
CHEMBL32392 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE IC50 = 1.0 nM 9.00
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE IC50 = 2.5 nM 8.60
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE IC50 = 5.0 nM 8.30
CHEMBL19130 IC50 = 10.0 nM 8.00
CHEMBL35556 IC50 = 24.0 nM 7.62
CHEMBL285414 IC50 = 25.0 nM 7.60
CHEMBL288096 IC50 = 25.0 nM 7.60
CHEMBL286787 IC50 = 25.0 nM 7.60
CHEMBL284248 IC50 = 30.0 nM 7.52
CHEMBL27559 IC50 = 36.0 nM 7.44
CHEMBL36061 IC50 = 112.0 nM 6.95
CHEMBL32330 IC50 = 143.0 nM 6.84
CHEMBL286929 IC50 = 204.0 nM 6.69
CHEMBL283871 IC50 = 394.0 nM 6.41
CHEMBL440846 IC50 = 700.0 nM 6.16
CHEMBL154709 APOCIDEINE IC50 = 2400.0 nM 5.62
CHEMBL284368 IC50 >= 5000.0 nM -
CHEMBL32392 IC50 > 10000.0 nM -