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Assay Detail

CHEMBL809261

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

Binding
Inhibition of [3H]5-HT reuptake at serotonin transporter in rat mid brain
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Zhang A, Zhou G, Rong SB, Johnson KM, Zhang M, Kozikowski AP.
Bioorg Med Chem Lett (2002) 12 : 993 -995
PubMed 11909701 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.05 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58858 1 10.22
CHEMBL58195 1 10.00
CHEMBL366383 1 8.81
CHEMBL119477 1 7.54
CHEMBL370805 COCAINE 4.0 1 6.81
CHEMBL173834 1 6.78
CHEMBL369497 1 6.77
CHEMBL117047 1 6.75
CHEMBL174854 1 5.94
CHEMBL367744 1 5.82
CHEMBL331565 1 5.69
CHEMBL366993 1 5.63
CHEMBL175338 1 4.88
CHEMBL173835 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58858 Ki = 0.06 nM 10.22
CHEMBL58195 Ki = 0.1 nM 10.00
CHEMBL366383 Ki = 1.53 nM 8.81
CHEMBL119477 Ki = 29.0 nM 7.54
CHEMBL370805 COCAINE Ki = 155.0 nM 6.81
CHEMBL173834 Ki = 168.0 nM 6.78
CHEMBL369497 Ki = 169.0 nM 6.77
CHEMBL117047 Ki = 179.0 nM 6.75
CHEMBL174854 Ki = 1150.0 nM 5.94
CHEMBL367744 Ki = 1530.0 nM 5.82
CHEMBL331565 Ki = 2046.0 nM 5.69
CHEMBL366993 Ki = 2360.0 nM 5.63
CHEMBL175338 Ki = 13300.0 nM 4.88
CHEMBL173835 Ki ~ 1000.0 nM -