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Assay Detail

CHEMBL4044354

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

Binding
Displacement of [3H]spiperone from human D2short receptor L2.64C mutant expressed in HEK293T 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
Cell Type HEK-293T
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.28 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100263 1 6.50
CHEMBL4086894 1 6.48
CHEMBL4065455 1 6.26
CHEMBL4082245 1 6.07
CHEMBL4071729 1 6.07
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100263 Ki = 320.0 nM 6.50
CHEMBL4086894 Ki = 330.0 nM 6.48
CHEMBL4065455 Ki = 550.0 nM 6.26
CHEMBL4082245 Ki = 850.0 nM 6.07
CHEMBL4071729 Ki = 860.0 nM 6.07
CHEMBL54 HALOPERIDOL Ki - -