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Assay Detail

CHEMBL673645

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Binding
Effective concentration against human Dopamine receptor D4
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Stewart AO, Cowart MD, Moreland RB, Latshaw SP, Matulenko MA, Bhatia PA, Wang X, Daanen JF, Nelson SL, Terranova MA, Namovic MT, Donnelly-Roberts DL, Miller LN, Nakane M, Sullivan JP, Brioni JD.
J Med Chem (2004) 47 : 2348 -2355
PubMed 15084133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.17 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77563 1 9.00
CHEMBL309372 1 8.25
CHEMBL77708 1 8.00
CHEMBL77395 1 7.50
CHEMBL310843 1 6.81
CHEMBL267014 L-745870 1 5.65
CHEMBL80469 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77563 EC50 = 1.0 nM 9.00
CHEMBL309372 EC50 = 5.6 nM 8.25
CHEMBL77708 EC50 = 10.1 nM 8.00
CHEMBL77395 EC50 = 32.0 nM 7.50
CHEMBL310843 EC50 = 154.0 nM 6.81
CHEMBL267014 L-745870 EC50 = 2230.0 nM 5.65
CHEMBL80469 EC50 = 10000.0 nM 5.00