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Assay Detail

CHEMBL3863992

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

Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
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
Ki 7 6.22 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3126735 1 7.55
CHEMBL8946 ETICLOPRIDE 2.0 1 7.15
CHEMBL11493 1 6.23
CHEMBL3918282 1 5.76
CHEMBL3931765 1 5.42
CHEMBL3916231 1 5.20
CHEMBL1201192 ARMODAFINIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3126735 Ki = 28.1 nM 7.55
CHEMBL8946 ETICLOPRIDE Ki = 70.4 nM 7.15
CHEMBL11493 Ki = 583.0 nM 6.23
CHEMBL3918282 Ki = 1750.0 nM 5.76
CHEMBL3931765 Ki = 3820.0 nM 5.42
CHEMBL3916231 Ki = 6300.0 nM 5.20
CHEMBL1201192 ARMODAFINIL Ki > 100000.0 nM -