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Assay Detail

CHEMBL674932

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Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.
DeNinno MP, Schoenleber R, Perner RJ, Lijewski L, Asin KE, Britton DR, MacKenzie R, Kebabian JW.
J Med Chem (1991) 34 : 2561 -2569
PubMed 1652023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.82 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314459 1 8.77
CHEMBL315468 1 8.15
CHEMBL313530 1 8.08
CHEMBL84983 1 7.72
CHEMBL420972 1 7.63
CHEMBL419680 1 7.52
CHEMBL86576 1 7.40
CHEMBL82899 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314459 EC50 = 1.7 nM 8.77
CHEMBL315468 EC50 = 7.1 nM 8.15
CHEMBL313530 EC50 = 8.3 nM 8.08
CHEMBL84983 EC50 = 18.9 nM 7.72
CHEMBL420972 EC50 = 23.4 nM 7.63
CHEMBL419680 EC50 = 30.3 nM 7.52
CHEMBL86576 EC50 = 39.8 nM 7.40
CHEMBL82899 EC50 = 52.3 nM 7.28