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Assay Detail

CHEMBL673578

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

Binding
Displacement of [3H]spiperone from rat striatal homogenate dopamine receptor D2
12
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 receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol.
Berger JG, Chang WK, Clader JW, Hou D, Chipkin RE, McPhail AT.
J Med Chem (1989) 32 : 1913 -1921
PubMed 2666667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.42 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298406 ECOPIPAM 3.0 1 6.29
CHEMBL58205 1 5.82
CHEMBL292451 1 5.61
CHEMBL58422 1 5.52
CHEMBL56666 2 5.46
CHEMBL59139 1 5.39
CHEMBL294215 1 5.19
CHEMBL294221 1 5.10
CHEMBL294012 1 4.79
CHEMBL442740 1 -
CHEMBL294186 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298406 ECOPIPAM Ki = 514.0 nM 6.29
CHEMBL58205 Ki = 1505.0 nM 5.82
CHEMBL292451 Ki = 2477.0 nM 5.61
CHEMBL58422 Ki = 3046.0 nM 5.52
CHEMBL56666 Ki = 3476.0 nM 5.46
CHEMBL59139 Ki = 4115.0 nM 5.39
CHEMBL294215 Ki = 6400.0 nM 5.19
CHEMBL294221 Ki = 7873.0 nM 5.10
CHEMBL56666 Ki = 9073.0 nM 5.04
CHEMBL294012 Ki = 16317.0 nM 4.79
CHEMBL442740 Ki > 100000.0 nM -
CHEMBL294186 Ki > 100000.0 nM -