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Assay Detail

CHEMBL673642

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

Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.
Glase SA, Akunne HC, Georgic LM, Heffner TG, MacKenzie RG, Manley PJ, Pugsley TA, Wise LD.
J Med Chem (1997) 40 : 1771 -1772
PubMed 9191952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.84 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300956 1 8.92
CHEMBL51023 1 8.47
CHEMBL49502 1 8.28
CHEMBL49231 1 8.08
CHEMBL296953 1 8.08
CHEMBL296506 1 7.89
CHEMBL48819 1 7.82
CHEMBL298166 1 7.80
CHEMBL45244 PD-168,077 1 7.77
CHEMBL423659 1 7.62
CHEMBL48807 1 7.51
CHEMBL298763 1 6.97
CHEMBL51536 1 6.66
CHEMBL49876 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300956 EC50 = 1.2 nM 8.92
CHEMBL51023 EC50 = 3.4 nM 8.47
CHEMBL49502 EC50 = 5.3 nM 8.28
CHEMBL49231 EC50 = 8.4 nM 8.08
CHEMBL296953 EC50 = 8.4 nM 8.08
CHEMBL296506 EC50 = 13.0 nM 7.89
CHEMBL48819 EC50 = 15.0 nM 7.82
CHEMBL298166 EC50 = 16.0 nM 7.80
CHEMBL45244 PD-168,077 EC50 = 17.0 nM 7.77
CHEMBL423659 EC50 = 24.0 nM 7.62
CHEMBL48807 EC50 = 31.0 nM 7.51
CHEMBL298763 EC50 = 106.0 nM 6.97
CHEMBL51536 EC50 = 218.0 nM 6.66
CHEMBL49876 EC50 > 3.9 nM -