Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3863998

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

Binding
Displacement of [3H]WIN35,428 from human DAT Y156F mutant expressed in COS7 cell membranes incubated for >90 mins by radioligand binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 9 5.85 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3918282 1 7.01
CHEMBL11493 1 6.58
CHEMBL3916231 1 6.57
CHEMBL370805 COCAINE 4.0 1 6.49
CHEMBL3126735 1 5.69
CHEMBL1672355 (S)-MODAFINIL 1 5.23
CHEMBL1201192 ARMODAFINIL 4.0 1 5.05
CHEMBL3931765 1 5.04
CHEMBL1373 MODAFINIL 4.0 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3918282 Ki = 97.0 nM 7.01
CHEMBL11493 Ki = 260.0 nM 6.58
CHEMBL3916231 Ki = 267.0 nM 6.57
CHEMBL370805 COCAINE Ki = 321.0 nM 6.49
CHEMBL3126735 Ki = 2050.0 nM 5.69
CHEMBL1672355 (S)-MODAFINIL Ki = 5910.0 nM 5.23
CHEMBL1201192 ARMODAFINIL Ki = 8920.0 nM 5.05
CHEMBL3931765 Ki = 9170.0 nM 5.04
CHEMBL1373 MODAFINIL Ki = 9250.0 nM 5.03