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Assay Detail

CHEMBL670137

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

Binding
Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL3998)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
Sonesson C, Waters N, Svensson K, Carlsson A, Smith MW, Piercey MF, Meier E, Wikström H.
J Med Chem (1993) 36 : 3188 -3196
PubMed 8230107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.12 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.52
CHEMBL278751 1 7.75
CHEMBL276500 2 6.86
CHEMBL27441 1 6.80
CHEMBL90359 1 6.75
CHEMBL107492 2 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.3 nM 9.52
CHEMBL278751 Ki = 18.0 nM 7.75
CHEMBL276500 Ki = 137.0 nM 6.86
CHEMBL27441 Ki = 158.0 nM 6.80
CHEMBL90359 Ki = 180.0 nM 6.75
CHEMBL276500 Ki = 776.0 nM 6.11
CHEMBL107492 Ki = 889.0 nM 6.05
CHEMBL107492 Ki > 2000.0 nM -