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Assay Detail

CHEMBL3863993

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in whole-guinea pig brain minus cerebellum homogenates incubated for 120 mins by radioligand binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 7.26 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11493 1 8.62
CHEMBL3916231 1 8.39
CHEMBL3126735 1 6.80
CHEMBL3918282 1 6.47
CHEMBL3931765 1 6.00
CHEMBL1201192 ARMODAFINIL 4.0 1 -
CHEMBL8946 ETICLOPRIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11493 Ki = 2.4 nM 8.62
CHEMBL3916231 Ki = 4.03 nM 8.39
CHEMBL3126735 Ki = 159.0 nM 6.80
CHEMBL3918282 Ki = 336.0 nM 6.47
CHEMBL3931765 Ki = 1010.0 nM 6.00
CHEMBL1201192 ARMODAFINIL Ki > 100000.0 nM -
CHEMBL8946 ETICLOPRIDE Ki - -