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Assay Detail

CHEMBL671376

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Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D2 in CHO cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
Zhang X, Hodgetts K, Rachwal S, Zhao H, Wasley JW, Craven K, Brodbeck R, Kieltyka A, Hoffman D, Bacolod MD, Girard B, Tran J, Thurkauf A.
J Med Chem (2000) 43 : 3923 -3932
PubMed 11052797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.37 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.15
CHEMBL1202208 1 7.21
CHEMBL1204116 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 7.0 nM 8.15
CHEMBL1202208 Ki = 61.0 nM 7.21
CHEMBL1204116 Ki = 181.0 nM 6.74