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Assay Detail

CHEMBL672750

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

Binding
Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum
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

Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Liao Y, DeBoer P, Meier E, Wikström H.
J Med Chem (1997) 40 : 4146 -4153
PubMed 9406603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.52 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.12
CHEMBL415300 ISOCLOZAPINE 1 7.89
CHEMBL72292 1 7.51
CHEMBL72794 1 7.17
CHEMBL42 CLOZAPINE 4.0 1 6.48
CHEMBL308090 1 5.89
CHEMBL73074 1 5.37
CHEMBL70377 1 5.19
CHEMBL310712 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL IC50 = 7.5 nM 8.12
CHEMBL415300 ISOCLOZAPINE IC50 = 13.0 nM 7.89
CHEMBL72292 IC50 = 31.0 nM 7.51
CHEMBL72794 IC50 = 68.0 nM 7.17
CHEMBL42 CLOZAPINE IC50 = 330.0 nM 6.48
CHEMBL308090 IC50 = 1300.0 nM 5.89
CHEMBL73074 IC50 = 4300.0 nM 5.37
CHEMBL70377 IC50 = 6400.0 nM 5.19
CHEMBL310712 IC50 = 8100.0 nM 5.09