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Assay Detail

CHEMBL4044353

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

Binding
Displacement of [3H]spiperone from human D2short receptor expressed in CHO cell membranes by radioligand binding assay
6
Total Activities
6
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

Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.
Schwalbe T, Kaindl J, Hübner H, Gmeiner P.
Bioorg Med Chem (2017) 25 : 5084 -5094
PubMed 28666858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.88 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.60
CHEMBL4086894 1 7.14
CHEMBL4100263 1 6.85
CHEMBL4082245 1 6.03
CHEMBL4065455 1 5.82
CHEMBL4071729 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.25 nM 9.60
CHEMBL4086894 Ki = 73.0 nM 7.14
CHEMBL4100263 Ki = 140.0 nM 6.85
CHEMBL4082245 Ki = 940.0 nM 6.03
CHEMBL4065455 Ki = 1500.0 nM 5.82
CHEMBL4071729 Ki = 1500.0 nM 5.82