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Assay Detail

CHEMBL672659

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Binding
Binding affinity against Dopamine receptor D2 using [3H]spiroperidol
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition.
Liljefors T, Bøgesø KP.
J Med Chem (1988) 31 : 306 -312
PubMed 2892932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.06 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303313 1 8.35
CHEMBL104911 1 8.22
CHEMBL1255588 1 7.92
CHEMBL95636 TEFLUDAZINE 2.0 1 7.85
CHEMBL64875 1 7.40
CHEMBL105013 1 6.23
CHEMBL320656 DEXCLAMOL 2.0 1 6.05
CHEMBL6066837 (-)-BUTACLAMOL 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303313 IC50 = 4.5 nM 8.35
CHEMBL104911 IC50 = 6.0 nM 8.22
CHEMBL1255588 IC50 = 12.0 nM 7.92
CHEMBL95636 TEFLUDAZINE IC50 = 14.0 nM 7.85
CHEMBL64875 IC50 = 40.0 nM 7.40
CHEMBL105013 IC50 = 590.0 nM 6.23
CHEMBL320656 DEXCLAMOL IC50 = 900.0 nM 6.05
CHEMBL6066837 (-)-BUTACLAMOL IC50 = 34000.0 nM 4.47