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Assay Detail

CHEMBL674492

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

Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.
Bergauer M, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2002) 12 : 1937 -1940
PubMed 12113813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.75 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7927 FAUC 113 1 8.51
CHEMBL57176 1 8.23
CHEMBL60815 1 7.92
CHEMBL42 CLOZAPINE 4.0 1 7.80
CHEMBL2113718 1 7.75
CHEMBL56118 1 7.68
CHEMBL58662 1 7.08
CHEMBL294394 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7927 FAUC 113 Ki = 3.1 nM 8.51
CHEMBL57176 Ki = 5.9 nM 8.23
CHEMBL60815 Ki = 12.0 nM 7.92
CHEMBL42 CLOZAPINE Ki = 16.0 nM 7.80
CHEMBL2113718 Ki = 18.0 nM 7.75
CHEMBL56118 Ki = 21.0 nM 7.68
CHEMBL58662 Ki = 83.0 nM 7.08
CHEMBL294394 Ki = 100.0 nM 7.00