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Assay Detail

CHEMBL1031545

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

Binding
Displacement of [125I]RTI55 from human DAT expressed in HEK cells
36
Total Activities
35
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

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.
Voelker T, Xia H, Fandrick K, Johnson R, Janowsky A, Cashman JR.
Bioorg Med Chem (2009) 17 : 2047 -2068
PubMed 19201198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 5.09 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 1 6.43
CHEMBL504028 1 6.29
CHEMBL458639 1 6.04
CHEMBL456639 1 5.82
CHEMBL460204 1 5.47
CHEMBL455221 1 5.41
CHEMBL459367 1 5.34
CHEMBL457966 1 5.26
CHEMBL461268 1 5.21
CHEMBL457968 1 5.20
CHEMBL462311 1 5.19
CHEMBL447825 1 5.17
CHEMBL450907 2 5.14
CHEMBL460407 1 5.13
CHEMBL456638 1 5.07
CHEMBL511500 1 4.84
CHEMBL460406 1 4.79
CHEMBL456221 1 4.57
CHEMBL456223 1 4.52
CHEMBL512736 1 4.48
CHEMBL450769 1 4.46
CHEMBL457967 1 4.37
CHEMBL456222 1 4.29
CHEMBL450987 1 4.01
CHEMBL456017 1 -
CHEMBL442843 1 -
CHEMBL451837 1 -
CHEMBL448912 1 -
CHEMBL508678 1 -
CHEMBL452928 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE Ki = 371.0 nM 6.43
CHEMBL504028 Ki = 512.0 nM 6.29
CHEMBL458639 Ki = 916.0 nM 6.04
CHEMBL456639 Ki = 1505.0 nM 5.82
CHEMBL460204 Ki = 3387.0 nM 5.47
CHEMBL455221 Ki = 3868.0 nM 5.41
CHEMBL459367 Ki = 4576.0 nM 5.34
CHEMBL457966 Ki = 5498.0 nM 5.26
CHEMBL461268 Ki = 6117.0 nM 5.21
CHEMBL457968 Ki = 6376.0 nM 5.20
CHEMBL462311 Ki = 6500.0 nM 5.19
CHEMBL447825 Ki = 6830.0 nM 5.17
CHEMBL450907 Ki = 7307.0 nM 5.14
CHEMBL460407 Ki = 7328.0 nM 5.13
CHEMBL456638 Ki = 8519.0 nM 5.07
CHEMBL511500 Ki = 14500.0 nM 4.84
CHEMBL460406 Ki = 16370.0 nM 4.79
CHEMBL450907 Ki = 21190.0 nM 4.67
CHEMBL456221 Ki = 27240.0 nM 4.57
CHEMBL456223 Ki = 30320.0 nM 4.52
CHEMBL512736 Ki = 32940.0 nM 4.48
CHEMBL450769 Ki = 34790.0 nM 4.46
CHEMBL457967 Ki = 42760.0 nM 4.37
CHEMBL456222 Ki = 51020.0 nM 4.29
CHEMBL450987 Ki = 97180.0 nM 4.01
CHEMBL459391 Ki > 10000.0 nM -
CHEMBL459390 Ki > 10000.0 nM -
CHEMBL451652 Ki > 10000.0 nM -
CHEMBL447750 Ki > 10000.0 nM -
CHEMBL511163 Ki > 10000.0 nM -
CHEMBL452928 Ki > 10000.0 nM -
CHEMBL508678 Ki > 10000.0 nM -
CHEMBL448912 Ki > 10000.0 nM -
CHEMBL451837 Ki > 10000.0 nM -
CHEMBL442843 Ki > 10000.0 nM -
CHEMBL456017 Ki > 10000.0 nM -