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Assay Detail

CHEMBL673629

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Binding
Binding affinity towards Dopamine receptor D2 by displacing [3H]spiperone
9
Total Activities
9
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 9 10.05 10.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135722 1 10.33
CHEMBL136942 1 10.24
CHEMBL135500 1 10.20
CHEMBL134545 1 10.17
CHEMBL335606 1 10.06
CHEMBL267932 MESPIPERONE 2.0 1 9.93
CHEMBL337181 1 9.92
CHEMBL135860 1 9.92
CHEMBL335714 1 9.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135722 Ki = 0.047 nM 10.33
CHEMBL136942 Ki = 0.057 nM 10.24
CHEMBL135500 Ki = 0.063 nM 10.20
CHEMBL134545 Ki = 0.067 nM 10.17
CHEMBL335606 Ki = 0.087 nM 10.06
CHEMBL267932 MESPIPERONE Ki = 0.118 nM 9.93
CHEMBL337181 Ki = 0.119 nM 9.92
CHEMBL135860 Ki = 0.12 nM 9.92
CHEMBL335714 Ki = 0.213 nM 9.67