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Assay Detail

CHEMBL893355

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

Functional
Inhibition of [3H]DA uptake in human NET expressed in COS1 cell membrane
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
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 33 5.51 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242338 IODINE 2BETA-CARBOMETHOXY-3BETA-(4 IODOPHENYL)-TROPANE -1.0 1 8.00
CHEMBL370805 COCAINE 4.0 1 6.74
CHEMBL232299 1 5.41
CHEMBL233088 1 5.33
CHEMBL395910 1 5.31
CHEMBL232068 1 5.00
CHEMBL398009 1 4.70
CHEMBL396082 1 4.58
CHEMBL245061 1 4.55
CHEMBL232663 1 -
CHEMBL232879 1 -
CHEMBL396318 1 -
CHEMBL434959 1 -
CHEMBL103936 1 -
CHEMBL394585 1 -
CHEMBL232671 1 -
CHEMBL232672 1 -
CHEMBL232867 1 -
CHEMBL232674 1 -
CHEMBL396083 1 -
CHEMBL232866 1 -
CHEMBL397787 1 -
CHEMBL232675 1 -
CHEMBL232069 1 -
CHEMBL232070 1 -
CHEMBL397520 1 -
CHEMBL234127 1 -
CHEMBL234128 1 -
CHEMBL232498 1 -
CHEMBL438321 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242338 IODINE 2BETA-CARBOMETHOXY-3BETA-(4 IODOPHENYL)-TROPANE Ki = 10.0 nM 8.00
CHEMBL370805 COCAINE Ki = 182.0 nM 6.74
CHEMBL232299 Ki = 3900.0 nM 5.41
CHEMBL233088 Ki = 4720.0 nM 5.33
CHEMBL395910 Ki = 4900.0 nM 5.31
CHEMBL232068 Ki = 10000.0 nM 5.00
CHEMBL398009 Ki = 20000.0 nM 4.70
CHEMBL396082 Ki = 26000.0 nM 4.58
CHEMBL245061 Ki = 28000.0 nM 4.55
CHEMBL232879 Ki - -
CHEMBL395649 Ki = 499000.0 nM -
CHEMBL396318 Ki - -
CHEMBL434959 Ki - -
CHEMBL103936 Ki - -
CHEMBL394585 Ki = 178000.0 nM -
CHEMBL232671 Ki = 285000.0 nM -
CHEMBL232672 Ki = 1390000.0 nM -
CHEMBL232867 Ki = 646000.0 nM -
CHEMBL232674 Ki = 247000.0 nM -
CHEMBL232870 Ki = 314000.0 nM -
CHEMBL231858 Ki = 871000.0 nM -
CHEMBL232663 Ki - -
CHEMBL396083 Ki - -
CHEMBL232866 Ki - -
CHEMBL397787 Ki - -
CHEMBL232675 Ki - -
CHEMBL232069 Ki - -
CHEMBL232070 Ki - -
CHEMBL397520 Ki - -
CHEMBL234127 Ki - -
CHEMBL234128 Ki - -
CHEMBL232498 Ki - -
CHEMBL438321 Ki - -