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Assay Detail

CHEMBL879549

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

Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and molecular modeling of 1-phenyl-1,2,3,4-tetrahydroisoquinolines and related 5,6,8,9-tetrahydro-13bH-dibenzo[a,h]quinolizines as D1 dopamine antagonists.
Minor DL, Wyrick SD, Charifson PS, Watts VJ, Nichols DE, Mailman RB.
J Med Chem (1994) 37 : 4317 -4328
PubMed 7996543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.76 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60706 1 6.54
CHEMBL135318 1 6.54
CHEMBL299056 1 6.28
CHEMBL62 SCH-23390 1 6.17
CHEMBL334350 1 5.89
CHEMBL303993 1 5.73
CHEMBL300778 1 5.72
CHEMBL57988 1 5.44
CHEMBL293158 1 4.72
CHEMBL446396 1 4.58
CHEMBL434809 1 -
CHEMBL137420 1 -
CHEMBL109723 1 -
CHEMBL323771 1 -
CHEMBL445129 1 -
CHEMBL336218 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60706 Ki = 287.0 nM 6.54
CHEMBL135318 Ki = 290.0 nM 6.54
CHEMBL299056 Ki = 522.0 nM 6.28
CHEMBL62 SCH-23390 Ki = 676.0 nM 6.17
CHEMBL334350 Ki = 1300.0 nM 5.89
CHEMBL303993 Ki = 1850.0 nM 5.73
CHEMBL300778 Ki = 1900.0 nM 5.72
CHEMBL57988 Ki = 3620.0 nM 5.44
CHEMBL293158 Ki = 19200.0 nM 4.72
CHEMBL446396 Ki = 26300.0 nM 4.58
CHEMBL434809 Ki > 5000.0 nM -
CHEMBL137420 Ki > 5000.0 nM -
CHEMBL109723 Ki > 5000.0 nM -
CHEMBL323771 Ki > 5000.0 nM -
CHEMBL445129 Ki > 5000.0 nM -
CHEMBL336218 Ki > 3000.0 nM -