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Assay Detail

CHEMBL5539185

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

Binding
Displacement of [3H]WIN35428 from human DAT Y156F mutant expessed in COS-7 cells incubated for 1.5 hrs by beta scintillation counting analysis
8
Total Activities
8
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

Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile.
Okorom AV, Camacho-Hernandez GA, Salomon K, Lee KH, Ku TC, Cao J, Won SJ, Friedman J, Lam J, Paule J, Rais R, Klein B, Xi ZX, Shi L, Loland CJ, Newman AH.
J Med Chem (2024) 67 : 709 -727
PubMed 38117239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.23 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3918282 1 6.94
CHEMBL5592085 1 6.74
CHEMBL5569659 1 6.63
CHEMBL370805 COCAINE 4.0 1 6.49
CHEMBL5572067 1 6.41
CHEMBL3084652 1 5.90
CHEMBL5571533 1 5.63
CHEMBL3931765 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3918282 Ki = 116.0 nM 6.94
CHEMBL5592085 Ki = 184.0 nM 6.74
CHEMBL5569659 Ki = 232.0 nM 6.63
CHEMBL370805 COCAINE Ki = 326.0 nM 6.49
CHEMBL5572067 Ki = 393.0 nM 6.41
CHEMBL3084652 Ki = 1250.0 nM 5.90
CHEMBL5571533 Ki = 2360.0 nM 5.63
CHEMBL3931765 Ki = 7560.0 nM 5.12