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Assay Detail

CHEMBL893351

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

Binding
Displacement of [125I]RTI55 from human SERT expressed in COS1 cell membrane
50
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.
Petersen MD, Boye SV, Nielsen EH, Willumsen J, Sinning S, Wiborg O, Bols M.
Bioorg Med Chem (2007) 15 : 4159 -4174
PubMed 17446076 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 5.54 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242338 IODINE 2BETA-CARBOMETHOXY-3BETA-(4 IODOPHENYL)-TROPANE -1.0 1 8.22
CHEMBL243141 1 6.66
CHEMBL215988 1 6.54
CHEMBL388257 1 6.36
CHEMBL370805 COCAINE 4.0 1 6.01
CHEMBL397490 2 5.73
CHEMBL242920 1 5.55
CHEMBL396754 1 5.52
CHEMBL243204 1 4.57
CHEMBL232879 1 4.54
CHEMBL232299 1 4.50
CHEMBL388255 1 4.33
CHEMBL231684 1 4.14
CHEMBL396318 1 -
CHEMBL434959 1 -
CHEMBL232498 1 -
CHEMBL232069 1 -
CHEMBL233532 1 -
CHEMBL394089 1 -
CHEMBL442234 1 -
CHEMBL233530 1 -
CHEMBL393701 1 -
CHEMBL394373 1 -
CHEMBL234379 1 -
CHEMBL232663 1 -
CHEMBL396083 1 -
CHEMBL394585 1 -
CHEMBL245061 1 -
CHEMBL103936 1 -
CHEMBL232671 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242338 IODINE 2BETA-CARBOMETHOXY-3BETA-(4 IODOPHENYL)-TROPANE Ki = 6.0 nM 8.22
CHEMBL243141 Ki = 217.0 nM 6.66
CHEMBL215988 Ki = 287.0 nM 6.54
CHEMBL388257 Ki = 440.0 nM 6.36
CHEMBL370805 COCAINE Ki = 965.0 nM 6.01
CHEMBL397490 Ki = 1850.0 nM 5.73
CHEMBL242920 Ki = 2810.0 nM 5.55
CHEMBL396754 Ki = 3000.0 nM 5.52
CHEMBL397490 Ki = 13800.0 nM 4.86
CHEMBL243204 Ki = 27000.0 nM 4.57
CHEMBL232879 Ki = 28700.0 nM 4.54
CHEMBL232299 Ki = 32000.0 nM 4.50
CHEMBL388255 Ki = 46700.0 nM 4.33
CHEMBL231684 Ki = 73000.0 nM 4.14
CHEMBL233088 Ki = 149000.0 nM -
CHEMBL396083 Ki = 1460000.0 nM -
CHEMBL395649 Ki = 573000.0 nM -
CHEMBL438321 Ki = 4710000.0 nM -
CHEMBL234128 Ki = 5020000.0 nM -
CHEMBL234127 Ki = 668000.0 nM -
CHEMBL397520 Ki = 4680000.0 nM -
CHEMBL232070 Ki = 2250000.0 nM -
CHEMBL396082 Ki = 417000.0 nM -
CHEMBL232068 Ki = 109000.0 nM -
CHEMBL231858 Ki = 1180000.0 nM -
CHEMBL232870 Ki = 1860000.0 nM -
CHEMBL395910 Ki = 228000.0 nM -
CHEMBL232675 Ki = 1141000.0 nM -
CHEMBL232674 Ki = 1950000.0 nM -
CHEMBL232867 Ki = 296000.0 nM -
CHEMBL397787 Ki = 3388000.0 nM -
CHEMBL232866 Ki = 3800000.0 nM -
CHEMBL393701 Ki = 1910000.0 nM -
CHEMBL232671 Ki = 2240000.0 nM -
CHEMBL103936 Ki = 620000.0 nM -
CHEMBL245061 Ki = 785000.0 nM -
CHEMBL394585 Ki = 2840000.0 nM -
CHEMBL232672 Ki = 2690000.0 nM -
CHEMBL232663 Ki = 1040000.0 nM -
CHEMBL234379 Ki = 1800000.0 nM -
CHEMBL394373 Ki = 185000.0 nM -
CHEMBL398009 Ki = 706000.0 nM -
CHEMBL233530 Ki = 1510000.0 nM -
CHEMBL442234 Ki = 605000.0 nM -
CHEMBL394089 Ki = 9120000.0 nM -
CHEMBL233532 Ki = 390000.0 nM -
CHEMBL232069 Ki = 841000.0 nM -
CHEMBL232498 Ki = 381000.0 nM -
CHEMBL434959 Ki = 532000.0 nM -
CHEMBL396318 Ki = 463000.0 nM -