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Assay Detail

CHEMBL4345340

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

Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
16
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL2056)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.
Park H, Urs AN, Zimmerman J, Liu C, Wang Q, Urs NM.
ACS Med Chem Lett (2020) 11 : 385 -392
PubMed 32184974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.72 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62 SCH-23390 2 8.16
CHEMBL4564103 2 5.41
CHEMBL4579687 2 5.29
CHEMBL4513262 2 5.13
CHEMBL4439029 2 5.07
CHEMBL4467483 2 4.83
CHEMBL4442011 2 -
CHEMBL4589737 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62 SCH-23390 IC50 = 6.918 nM 8.16
CHEMBL62 SCH-23390 IC50 = 6.96 nM 8.16
CHEMBL4564103 IC50 = 3890.45 nM 5.41
CHEMBL4564103 IC50 = 3887.0 nM 5.41
CHEMBL4579687 IC50 = 5128.61 nM 5.29
CHEMBL4579687 IC50 = 5115.0 nM 5.29
CHEMBL4513262 IC50 = 7413.1 nM 5.13
CHEMBL4513262 IC50 = 7461.0 nM 5.13
CHEMBL4439029 IC50 = 8511.38 nM 5.07
CHEMBL4439029 IC50 = 8590.0 nM 5.07
CHEMBL4467483 IC50 = 14791.08 nM 4.83
CHEMBL4442011 IC50 > 10000.0 nM -
CHEMBL4589737 IC50 > 10000.0 nM -
CHEMBL4467483 IC50 > 10000.0 nM -
CHEMBL4442011 IC50 > 10000.0 nM -
CHEMBL4589737 IC50 > 10000.0 nM -