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Assay Detail

CHEMBL673444

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Binding
Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone
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(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
Löber S, Hübner H, Utz W, Gmeiner P.
J Med Chem (2001) 44 : 2691 -2694
PubMed 11495580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.17 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 6.02
CHEMBL432059 1 5.31
CHEMBL7927 FAUC 113 1 5.30
CHEMBL310843 1 5.28
CHEMBL88937 1 5.00
CHEMBL90374 1 4.92
CHEMBL91362 1 4.92
CHEMBL328925 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 960.0 nM 6.02
CHEMBL432059 Ki = 4900.0 nM 5.31
CHEMBL7927 FAUC 113 Ki = 5000.0 nM 5.30
CHEMBL310843 Ki = 5300.0 nM 5.28
CHEMBL88937 Ki = 10000.0 nM 5.00
CHEMBL90374 Ki = 12000.0 nM 4.92
CHEMBL91362 Ki = 12000.0 nM 4.92
CHEMBL328925 Ki = 23000.0 nM 4.64