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Assay Detail

CHEMBL828863

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

Binding
Inhibition of [3H]spiperone binding to rat dopamine D2 receptor
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

Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
Campiani G, Butini S, Fattorusso C, Trotta F, Gemma S, Catalanotti B, Nacci V, Fiorini I, Cagnotto A, Mereghetti I, Mennini T, Minetti P, Di Cesare MA, Stasi MA, Di Serio S, Ghirardi O, Tinti O, Carminati P.
J Med Chem (2005) 48 : 1705 -1708
PubMed 15771414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.41 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426763 1 9.37
CHEMBL54 HALOPERIDOL 4.0 1 8.32
CHEMBL180319 1 8.08
CHEMBL367045 1 7.76
CHEMBL715 OLANZAPINE 4.0 1 7.16
CHEMBL179557 1 7.15
CHEMBL42 CLOZAPINE 4.0 1 6.60
CHEMBL179775 1 6.24
CHEMBL178564 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426763 Ki = 0.43 nM 9.37
CHEMBL54 HALOPERIDOL Ki = 4.8 nM 8.32
CHEMBL180319 Ki = 8.4 nM 8.08
CHEMBL367045 Ki = 17.2 nM 7.76
CHEMBL715 OLANZAPINE Ki = 69.0 nM 7.16
CHEMBL179557 Ki = 71.1 nM 7.15
CHEMBL42 CLOZAPINE Ki = 250.0 nM 6.60
CHEMBL179775 Ki = 578.0 nM 6.24
CHEMBL178564 Ki = 923.0 nM 6.04