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Assay Detail

CHEMBL4397361

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ADMET
Agonist activity at recombinant human D2 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D<sub>3</sub> Receptor (D<sub>3</sub>R) Ligand Promiscuity across Highly Conserved Aminergic G-Protein-Coupled Receptors (GPCRs).
Reilly SW, Riad AA, Hsieh CJ, Sahlholm K, Jacome DA, Griffin S, Taylor M, Weng CC, Xu K, Kirschner N, Luedtke RR, Parry C, Malhotra S, Karanicolas J, Mach RH.
J Med Chem (2019) 62 : 5132 -5147
PubMed 31021617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.76 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240773 QUINPIROLE 2.0 1 8.92
CHEMBL4083252 1 6.59
CHEMBL4084262 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240773 QUINPIROLE EC50 = 1.2 nM 8.92
CHEMBL4083252 EC50 = 254.0 nM 6.59
CHEMBL4084262 EC50 - -