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Assay Detail

CHEMBL673090

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

Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D2L expressed in CHO K-1 cells
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).
van Vliet LA, Rodenhuis N, Dijkstra D, Wikström H, Pugsley TA, Serpa KA, Meltzer LT, Heffner TG, Wise LD, Lajiness ME, Huff RM, Svensson K, Sundell S, Lundmark M.
J Med Chem (2000) 43 : 2871 -2882
PubMed 10956195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.10 6.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330216 1 6.27
CHEMBL70565 2 5.93
CHEMBL97424 1 -
CHEMBL317493 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330216 Ki = 533.0 nM 6.27
CHEMBL70565 Ki = 1180.0 nM 5.93
CHEMBL97424 Ki > 10000.0 nM -
CHEMBL317493 Ki > 10000.0 nM -
CHEMBL70565 Ki > 10000.0 nM -