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Assay Detail

CHEMBL817692

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

Binding
Ability to displace [3H]haloperidol from rat striatal membranes, in order to measure its intrinsic affinity for the dopamine (DA) receptor
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans.
Bøgesø KP.
J Med Chem (1983) 26 : 935 -947
PubMed 6134833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.31 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54661 Z-FLUPENTIXOL 1 8.52
CHEMBL64249 CLOROTEPINE 2.0 1 8.52
CHEMBL1204350 1 8.09
CHEMBL12628 1 8.06
CHEMBL71 CHLORPROMAZINE 4.0 1 7.92
CHEMBL2447954 1 7.89
CHEMBL1204382 1 7.68
CHEMBL1204285 4 7.66
CHEMBL1204347 1 7.37
CHEMBL1203891 1 7.32
CHEMBL1203868 1 7.19
CHEMBL1204381 1 6.82
CHEMBL433602 1 6.72
CHEMBL136562 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54661 Z-FLUPENTIXOL IC50 = 3.0 nM 8.52
CHEMBL64249 CLOROTEPINE IC50 = 3.0 nM 8.52
CHEMBL1204350 IC50 = 8.1 nM 8.09
CHEMBL12628 IC50 = 8.8 nM 8.06
CHEMBL71 CHLORPROMAZINE IC50 = 12.0 nM 7.92
CHEMBL2447954 IC50 = 13.0 nM 7.89
CHEMBL1204382 IC50 = 21.0 nM 7.68
CHEMBL1204285 IC50 = 22.0 nM 7.66
CHEMBL1204347 IC50 = 43.0 nM 7.37
CHEMBL1203891 IC50 = 48.0 nM 7.32
CHEMBL1204285 IC50 = 57.0 nM 7.24
CHEMBL1203868 IC50 = 64.0 nM 7.19
CHEMBL1204381 IC50 = 150.0 nM 6.82
CHEMBL433602 IC50 = 190.0 nM 6.72
CHEMBL1204285 IC50 = 780.0 nM 6.11
CHEMBL1204285 IC50 = 2500.0 nM 5.60
CHEMBL136562 IC50 = 3200.0 nM 5.50