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Assay Detail

CHEMBL673630

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

Binding
Displacement of [3H]spiperone from dopamine receptor D2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.
Mach RH, Jackson JR, Luedtke RR, Ivins KJ, Molinoff PB, Ehrenkaufer RL.
J Med Chem (1992) 35 : 423 -430
PubMed 1531364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 10.40 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134400 1 10.64
CHEMBL137648 1 10.64
CHEMBL135917 1 10.54
CHEMBL135832 1 10.48
CHEMBL337149 1 10.46
CHEMBL136852 1 10.44
CHEMBL334349 1 10.41
CHEMBL137309 1 10.37
CHEMBL267930 SPIPERONE 2.0 1 10.24
CHEMBL135316 1 10.21
CHEMBL344399 1 10.20
CHEMBL538404 1 10.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134400 Ki = 0.023 nM 10.64
CHEMBL137648 Ki = 0.023 nM 10.64
CHEMBL135917 Ki = 0.029 nM 10.54
CHEMBL135832 Ki = 0.033 nM 10.48
CHEMBL337149 Ki = 0.035 nM 10.46
CHEMBL136852 Ki = 0.036 nM 10.44
CHEMBL334349 Ki = 0.039 nM 10.41
CHEMBL137309 Ki = 0.043 nM 10.37
CHEMBL267930 SPIPERONE Ki = 0.058 nM 10.24
CHEMBL135316 Ki = 0.062 nM 10.21
CHEMBL344399 Ki = 0.063 nM 10.20
CHEMBL538404 Ki = 0.069 nM 10.16