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Assay Detail

CHEMBL678337

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

Binding
Inhibitory constant against binding of [125I]- IBZM to rat striatal membrane
8
Total Activities
8
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 Autocuration

Target

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

Publication

Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
Kung HF, Kasliwal R, Pan SG, Kung MP, Mach RH, Guo YZ.
J Med Chem (1988) 31 : 1039 -1043
PubMed 2966245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.79 9.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 9.83
CHEMBL267723 IOLOPRIDE 2.0 1 9.20
CHEMBL1255588 1 9.07
CHEMBL8674 1 7.52
CHEMBL8945 1 7.51
CHEMBL59 DOPAMINE 4.0 1 6.53
CHEMBL51 KETANSERIN 3.0 1 6.45
CHEMBL62 SCH-23390 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 0.149 nM 9.83
CHEMBL267723 IOLOPRIDE Ki = 0.633 nM 9.20
CHEMBL1255588 Ki = 0.851 nM 9.07
CHEMBL8674 Ki = 30.3 nM 7.52
CHEMBL8945 Ki = 31.1 nM 7.51
CHEMBL59 DOPAMINE Ki = 296.0 nM 6.53
CHEMBL51 KETANSERIN Ki = 359.0 nM 6.45
CHEMBL62 SCH-23390 Ki = 600.0 nM 6.22