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Assay Detail

CHEMBL912415

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Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
10
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.
Cueva JP, Giorgioni G, Grubbs RA, Chemel BR, Watts VJ, Nichols DE.
J Med Chem (2006) 49 : 6848 -6857
PubMed 17154515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.48 8.30
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240773 QUINPIROLE 2.0 1 8.30
CHEMBL59 DOPAMINE 4.0 1 8.00
CHEMBL25856 DIHYDREXIDINE 2.0 1 7.77
CHEMBL1203924 2 7.68
CHEMBL387250 1 7.02
CHEMBL217299 DOXANTHRINE 1 6.96
CHEMBL384046 1 6.64
CHEMBL71 CHLORPROMAZINE 4.0 1 -
CHEMBL62 SCH-23390 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240773 QUINPIROLE EC50 = 5.0 nM 8.30
CHEMBL59 DOPAMINE EC50 = 10.0 nM 8.00
CHEMBL25856 DIHYDREXIDINE EC50 = 17.0 nM 7.77
CHEMBL1203924 EC50 = 21.0 nM 7.68
CHEMBL387250 EC50 = 95.0 nM 7.02
CHEMBL217299 DOXANTHRINE EC50 = 110.0 nM 6.96
CHEMBL384046 EC50 = 230.0 nM 6.64
CHEMBL71 CHLORPROMAZINE EC50 - -
CHEMBL62 SCH-23390 EC50 - -
CHEMBL1203924 Activity - -