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Assay Detail

CHEMBL3863985

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

Binding
Displacement of [3H]WIN35,428 from DAT in Sprague-Dawley rat brain membranes incubated for 120 mins by radioligand binding assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 40 7.40 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3918282 1 8.60
CHEMBL3979590 1 8.60
CHEMBL3941865 1 8.54
CHEMBL3894678 1 8.50
CHEMBL3890247 1 8.46
CHEMBL3952924 1 8.45
CHEMBL3965237 1 8.35
CHEMBL3907263 1 8.30
CHEMBL3909363 1 8.17
CHEMBL3935199 1 8.13
CHEMBL3971463 1 8.12
CHEMBL3923939 1 8.02
CHEMBL11493 1 7.98
CHEMBL3916231 1 7.78
CHEMBL3931813 1 7.71
CHEMBL3959292 1 7.58
CHEMBL3904892 1 7.57
CHEMBL3927228 1 7.54
CHEMBL3889802 1 7.48
CHEMBL3890835 1 7.42
CHEMBL3895932 1 7.41
CHEMBL3899193 1 7.33
CHEMBL3944169 1 7.30
CHEMBL3957984 1 7.27
CHEMBL3944646 1 7.25
CHEMBL3979186 1 7.23
CHEMBL3970990 1 7.13
CHEMBL3126735 1 6.94
CHEMBL3950591 1 6.84
CHEMBL3908243 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3918282 Ki = 2.53 nM 8.60
CHEMBL3979590 Ki = 2.54 nM 8.60
CHEMBL3941865 Ki = 2.92 nM 8.54
CHEMBL3894678 Ki = 3.17 nM 8.50
CHEMBL3890247 Ki = 3.43 nM 8.46
CHEMBL3952924 Ki = 3.58 nM 8.45
CHEMBL3965237 Ki = 4.5 nM 8.35
CHEMBL3907263 Ki = 4.98 nM 8.30
CHEMBL3909363 Ki = 6.72 nM 8.17
CHEMBL3935199 Ki = 7.4 nM 8.13
CHEMBL3971463 Ki = 7.62 nM 8.12
CHEMBL3923939 Ki = 9.67 nM 8.02
CHEMBL11493 Ki = 10.5 nM 7.98
CHEMBL3916231 Ki = 16.7 nM 7.78
CHEMBL3931813 Ki = 19.3 nM 7.71
CHEMBL3959292 Ki = 26.6 nM 7.58
CHEMBL3904892 Ki = 27.2 nM 7.57
CHEMBL3927228 Ki = 28.6 nM 7.54
CHEMBL3889802 Ki = 33.0 nM 7.48
CHEMBL3890835 Ki = 37.6 nM 7.42
CHEMBL3895932 Ki = 39.4 nM 7.41
CHEMBL3899193 Ki = 47.2 nM 7.33
CHEMBL3944169 Ki = 49.6 nM 7.30
CHEMBL3957984 Ki = 53.7 nM 7.27
CHEMBL3944646 Ki = 56.3 nM 7.25
CHEMBL3979186 Ki = 58.7 nM 7.23
CHEMBL3970990 Ki = 74.3 nM 7.13
CHEMBL3126735 Ki = 116.0 nM 6.94
CHEMBL3950591 Ki = 143.0 nM 6.84
CHEMBL3908243 Ki = 214.0 nM 6.67
CHEMBL3936184 Ki = 277.0 nM 6.56
CHEMBL3899819 Ki = 279.0 nM 6.55
CHEMBL3931765 Ki = 289.0 nM 6.54
CHEMBL3900352 Ki = 403.0 nM 6.39
CHEMBL3913879 Ki = 636.0 nM 6.20
CHEMBL3925079 Ki = 752.0 nM 6.12
CHEMBL3961296 Ki = 915.0 nM 6.04
CHEMBL3916742 Ki = 1380.0 nM 5.86
CHEMBL1201192 ARMODAFINIL Ki = 3050.0 nM 5.52
CHEMBL8946 ETICLOPRIDE Ki - -