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Assay Detail

CHEMBL670364

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Binding
Inhibition of mouse Dopamine receptor D2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL3427)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
Norman MH, Navas F, Thompson JB, Rigdon GC.
J Med Chem (1996) 39 : 4692 -4703
PubMed 8941382 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.75 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343838 1 8.66
CHEMBL142850 1 8.24
CHEMBL143075 1 8.22
CHEMBL141392 1 8.11
CHEMBL141438 1 8.02
CHEMBL85 RISPERIDONE 4.0 1 7.64
CHEMBL344994 1 7.62
CHEMBL356743 1 7.55
CHEMBL343228 1 7.55
CHEMBL142277 1 7.47
CHEMBL356498 1 7.33
CHEMBL42 CLOZAPINE 4.0 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343838 IC50 = 2.2 nM 8.66
CHEMBL142850 IC50 = 5.8 nM 8.24
CHEMBL143075 IC50 = 6.0 nM 8.22
CHEMBL141392 IC50 = 7.8 nM 8.11
CHEMBL141438 IC50 = 9.6 nM 8.02
CHEMBL85 RISPERIDONE IC50 = 23.0 nM 7.64
CHEMBL344994 IC50 = 24.0 nM 7.62
CHEMBL356743 IC50 = 28.0 nM 7.55
CHEMBL343228 IC50 = 28.0 nM 7.55
CHEMBL142277 IC50 = 34.0 nM 7.47
CHEMBL356498 IC50 = 47.0 nM 7.33
CHEMBL42 CLOZAPINE IC50 = 290.0 nM 6.54