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Assay Detail

CHEMBL4345342

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

Functional
Antagonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
12
Total Activities
6
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(2) dopamine receptor (CHEMBL217)
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 12 6.78 9.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4467483 2 9.91
CHEMBL8809 RACLOPRIDE 2.0 2 7.00
CHEMBL4564103 2 6.44
CHEMBL4579687 2 5.49
CHEMBL4513262 2 5.05
CHEMBL4442011 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4467483 IC50 = 0.123 nM 9.91
CHEMBL4467483 IC50 = 0.124 nM 9.91
CHEMBL8809 RACLOPRIDE IC50 = 100.0 nM 7.00
CHEMBL8809 RACLOPRIDE IC50 = 104.2 nM 6.98
CHEMBL4564103 IC50 = 363.08 nM 6.44
CHEMBL4564103 IC50 = 365.2 nM 6.44
CHEMBL4579687 IC50 = 3235.94 nM 5.49
CHEMBL4579687 IC50 = 3222.0 nM 5.49
CHEMBL4513262 IC50 = 8912.51 nM 5.05
CHEMBL4513262 IC50 = 8900.0 nM 5.05
CHEMBL4442011 IC50 > 10000.0 nM -
CHEMBL4442011 IC50 > 10000.0 nM -