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Assay Detail

CHEMBL4430333

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

Binding
Displacement of [3H]spiperone from rat D2L dopamine receptor expressed in HEK293 cell membranes after 1 hr
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel multifunctional dopamine D<sub>2</sub>/D<sub>3</sub> receptors agonists with potential neuroprotection and anti-alpha synuclein protein aggregation properties.
Luo D, Sharma H, Yedlapudi D, Antonio T, Reith MEA, Dutta AK.
Bioorg Med Chem (2016) 24 : 5088 -5102
PubMed 27591013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.75 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4538230 1 8.33
CHEMBL4535160 1 7.23
CHEMBL4457171 1 7.18
CHEMBL4452046 1 7.17
CHEMBL4466245 1 6.95
CHEMBL4581614 1 6.94
CHEMBL4442119 1 6.93
CHEMBL4573578 1 6.91
CHEMBL273273 5-OH-DPAT 1 6.82
CHEMBL4456350 1 6.82
CHEMBL4558954 1 6.76
CHEMBL4442437 1 6.63
CHEMBL4535068 1 6.30
CHEMBL59 DOPAMINE 4.0 1 6.00
CHEMBL4549004 1 5.62
CHEMBL4593758 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4538230 Ki = 4.67 nM 8.33
CHEMBL4535160 Ki = 58.5 nM 7.23
CHEMBL4457171 Ki = 65.7 nM 7.18
CHEMBL4452046 Ki = 68.3 nM 7.17
CHEMBL4466245 Ki = 112.0 nM 6.95
CHEMBL4581614 Ki = 116.0 nM 6.94
CHEMBL4442119 Ki = 117.0 nM 6.93
CHEMBL4573578 Ki = 123.0 nM 6.91
CHEMBL273273 5-OH-DPAT Ki = 153.0 nM 6.82
CHEMBL4456350 Ki = 150.0 nM 6.82
CHEMBL4558954 Ki = 175.0 nM 6.76
CHEMBL4442437 Ki = 233.0 nM 6.63
CHEMBL4535068 Ki = 499.0 nM 6.30
CHEMBL59 DOPAMINE Ki = 990.0 nM 6.00
CHEMBL4549004 Ki = 2404.0 nM 5.62
CHEMBL4593758 Ki = 4634.0 nM 5.33