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Assay Detail

CHEMBL3757886

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

Binding
Displacement of [3H]N-methylspiperone from human cloned D2 dopamine receptor expressed in human fibroblasts incubated for 90 mins by scintillation counting based radioligand binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

D1-like receptors distinguishing thieno-azecine regioisomers
Abdel-Fattah MAO, Abadi AH, Lehmann J, Schweikert PM, Enzensperger C
Medchemcomm (2015) 6 : 1679 -1686
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.23 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3187365 ASENAPINE 4.0 1 8.05
CHEMBL715 OLANZAPINE 4.0 1 7.28
CHEMBL42 CLOZAPINE 4.0 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3187365 ASENAPINE Ki = 8.9 nM 8.05
CHEMBL715 OLANZAPINE Ki = 53.0 nM 7.28
CHEMBL42 CLOZAPINE Ki = 431.0 nM 6.37