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Assay Detail

CHEMBL676137

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

Binding
Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents.
Murphy RA, Kung HF, Kung MP, Billings J.
J Med Chem (1990) 33 : 171 -178
PubMed 2136916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.48 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 10.82
CHEMBL48450 1 10.07
CHEMBL267723 IOLOPRIDE 2.0 1 9.58
CHEMBL8809 RACLOPRIDE 2.0 1 8.96
CHEMBL1255588 1 8.92
CHEMBL301532 1 8.41
CHEMBL26736 1 7.18
CHEMBL51 KETANSERIN 3.0 1 6.31
CHEMBL59 DOPAMINE 4.0 1 6.07
CHEMBL27 PROPRANOLOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 0.015 nM 10.82
CHEMBL48450 Ki = 0.085 nM 10.07
CHEMBL267723 IOLOPRIDE Ki = 0.261 nM 9.58
CHEMBL8809 RACLOPRIDE Ki = 1.1 nM 8.96
CHEMBL1255588 Ki = 1.19 nM 8.92
CHEMBL301532 Ki = 3.89 nM 8.41
CHEMBL26736 Ki = 65.7 nM 7.18
CHEMBL51 KETANSERIN Ki = 491.0 nM 6.31
CHEMBL59 DOPAMINE Ki = 843.0 nM 6.07
CHEMBL27 PROPRANOLOL Ki > 10000.0 nM -