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Assay Detail

CHEMBL3863997

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

Binding
Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 10 mins by BRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.
Cao J, Slack RD, Bakare OM, Burzynski C, Rais R, Slusher BS, Kopajtic T, Bonifazi A, Ellenberger MP, Yano H, He Y, Bi GH, Xi ZX, Loland CJ, Newman AH.
J Med Chem (2016) 59 : 10676 -10691
PubMed 27933960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.19 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201192 ARMODAFINIL 4.0 1 8.68
CHEMBL3126735 1 5.70
CHEMBL11493 1 -
CHEMBL3916231 1 -
CHEMBL3931765 1 -
CHEMBL3918282 1 -
CHEMBL8946 ETICLOPRIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201192 ARMODAFINIL IC50 = 2.1 nM 8.68
CHEMBL3126735 IC50 = 2000.0 nM 5.70
CHEMBL11493 IC50 > 10000.0 nM -
CHEMBL3916231 IC50 > 10000.0 nM -
CHEMBL3931765 IC50 > 10000.0 nM -
CHEMBL3918282 IC50 > 10000.0 nM -
CHEMBL8946 ETICLOPRIDE IC50 > 10000.0 nM -